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Professor Michael Kassiou

BSc(Hons)PhD
Professor Michael Kassiou Associate Dean, Research and Innovation

C43A - Jeffrey Miller Admin Building Cumberland Campus
The University of Sydney

Telephone +61 2 9351 0849 BMRI
Fax +61 2 9351 0852 BMRI

Website Drug Discovery

Biographical details

Professor Michael Kassiou is an internationally recognized research leader in the chemistry of CNS bioactive drugs and has been responsible for fundamental contributions in drug discovery and a number of related areas which encompass the interface between chemistry and biology. His research is primarily concerned with the understanding of drug-protein and drug-binding site interactions in order to obtain structure-activity relationships of bioactive CNS molecules. This allows the rationale design of more efficacious treatments for diseases of the brain. In addition by using in vivo molecular imaging techniques within these fields we are better able to understand the functioning of the living brain and assess efficacy of newly developed treatments. He has held visiting appointments at The Johns Hopkins Medical Institutes USA and the SHFJ-CEA Life Sciences group in France. In 1996 he was awarded a Fogerty International Fellowship at the National Institutes of Health in the USA. He is the author of over 100 scientific research papers, reviews and book chapters and is a Fellow of the Royal Australian Chemical Institute (FRACI C.Chem.) He is a thematic editor for Current Pharmaceutical Design and the Editor for the Journal of Labelled Compounds and Radiopharmaceuticals. In addition, he serves on the 11 journal editorial advisory boards concerned with medicinal chemistry and drug design. He is a committee member of the Biomolecular Chemistry Division, member of the Australian Institute of Nuclear Science and Engineering - Biomedical Science and Biotechnology Committee, and board member of the Australian and French Association of Science (AFAS) NSW.

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Themes

Medical Imaging and Radiation Sciences; Neurosciences and Mental Health

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Selected grants

2013

  • Development of small molecule inhibitors of LRRK2 for treatment of Parkinson's disease; Kassiou M; Parkinson's New South Wales Incorporated/Research Support.
  • Development of small molecule inhibitors of LRRK2 for treatment of Parkinson's disease; Kassiou M; Parkinson's New South Wales Incorporated/Research Support.

2012

  • A flexible high throughput analytical system for psychopharmacology and drug discovery; McGregor I, Simpson S, Shannon Weickert C, Kassiou M, Copeland J, Solowij N, Codd R, Arnold J, Karl T, Long L; Australian Research Council/Linkage Infrastructure, Equipment and Facilities (LIEF).
  • A unique class of tumour-specific drugs for the trearment of advanced metastatic cancer; Rendina L, Kassiou M; National Breast Cancer Foundation/Novel Concept Awards.
  • New Strategies in the Treatment and Imaging of Neurodegenerative Diseases; Kassiou M; NHMRC/Australian-European Union (EU) Collaborative Grant.
  • Oxytocin receptor agonists for treatment of social anxiety; Kassiou M, McGregor I, Hunt G; National Health and Medical Research Council/Project Grants.

2011

  • Imaging of neuroinflammation in neurodegenerative disease (INMiND); Jacobs A, Maggi A, Aigner L, Guilloteau D, Aime S, Planas A, Van Der Linden A, Tavitian B, Herholz K, Boutin H, Perani D, Halldin C, Nordberg A, Van Laere K, Baekelandt V, Knudsen G, Pappata S, Rinne J, Holmes C, Roncaroli F, Brooks D, Kassiou M, Kellermayer M, Heneka M, Biserni A, Perk I, Cavallotti C, Alavijeh M, Mathe D, Ronn L; European Commission (Belgium)/Seventh Framework Network of Excellence Programme.
  • Preclinical validation of oxytocin as a novel treatment for alcohol dependence; McGregor I, Hunt G, Kassiou M; National Health and Medical Research Council/Project Grants.
  • The Development of Carboranes as New Agents in the Diagnosis and Treatment of Brain Disease; Kassiou M, Rendina L; Australian Research Council (ARC)/Discovery Projects (DP).
  • Preparative High-Performance Liquid Chromatography (HPLC); Payne R, Jolliffe K, Hambley T, Kassiou M, Collins (Chebib) M; National Health and Medical Research Council/Equipment Grants.
  • Molecular targets of amino acid/neurotransmitter conjugates of fatty acids; Connor M, Vaughan C, Kassiou M, McIntyre P; National Health and Medical Research Council/Project Grants.

2010

  • Purinergic P2X7 Receptor as a Target for Antidepressant Drug Discovery; Kassiou M, McGregor I, Bennett M; National Health and Medical Research Council/Project Grants.
  • The translocator protein (TSPO) as a novel target for the treatment of Alzheimer's Disease; Ittner L, Kassiou M; National Health and Medical Research Council/Project Grants.
  • Radiolabelled MMP Binding Agents for the Identification, Quantification, and Targeting of MMPs in CNS Disorders and Tumours; Hambley T, Kassiou M; Australian Research Council (ARC)/Discovery Projects (DP).

2009

  • Selective Targeting of Breast Tumours for Boron Neutron Capture Therapy; Rendina L, Kassiou M; National Breast Cancer Foundation/Novel Concept Awards.
  • Motion Menura multimodal mouse testing apparatus (MMTA): (Turnkey system comprising 6 testing chambers with associated control and tracking software).; Kemp A, Hermens D, McGregor I, Einfeld S, Kassiou M, Arnold J, Hunt G; National Health and Medical Research Council/Equipment Grants.

2008

  • RES: Contract Research Agreement with Bayer Schering Pharma; Kassiou M; Bayer Schering Pharma AG/Research Support.
  • The Targeting of Brain Tumours by a New Class of Agents for Boron Neutron Capture Therapy; Rendina L, Kassiou M; Cure Cancer Australia Foundation/Research Support.
  • Development of Novel Radiolabelled Molecular Probes for Studying Diseases of the Brain; Kassiou M; Department of Industry, Innovation, Science, Research and Tertiary Education (Federal)/International Science Linkages (ISL) Competitive Grants.

2007

  • Characterisation - Imaging; Meikle S, Kassiou M, Banati R; Office for Science and Medical Research (NSW)/National Collaborative Research Infrastructure Strategy Program.
  • Automatic Gamma Counter; Meikle S, Banati R, Kassiou M, Bailey D, Baldock C; NHMRC/Equipment Grant.
  • Development of Novel Radiolabelled Molecular Probes for Studying Diseases of the Brain; Meikle S, Banati R, Kassiou M; DEST/International Science Linkages Competitive Grants.
  • Evaluation of a selective NMDA NR1A/2B receptor antagonist as a drug treatment in an animal model of Parkinsons disease; Henderson J, Kassiou M; Australian Rotary Health Research Fund/Research Grant.
  • Establishment of a National Imaging Facility; Banati R, Meikle S, Kassiou M; Department of Education, Science and Training (DEST)/National Collaborative Research Infrastructure Strategy (Australia).

2006

  • Functionalised MMP Inhibitors as Radiodiagnostic, Radiotherapeutic, and Radiation-Sensitising Agents for Metastatic Cancer; Hambley T, Kassiou M; Australian Research Council (ARC)/Discovery Project.

2005

  • Functional in vivo imaging of neurodegenerative disorders of the brain using PET & SPECT; Kassiou M, Guilloteau D; DEST/Innovation Access Program.
  • Glial and neuroinflammatory mechanisms of neuronal degeneration and regeneration: The functional states of microglia in central nervous system and macrophages in the peripheral nervous system.; Pollard J, Kassiou M, Prineas J, Banati R, Bennett M; NSW Ministry of Science and Medical Research/Spinal Cord Injury Research Grants.
  • Evaluation of a selective NMDA NR1A/2B receptor antagonist as a drug treatment in an animal model of Parkinsons disease.; Henderson J, Kassiou M; Australian Rotary Health Research Fund/Parkinsons Disease.

2004

  • 1295 - Comparison of structurally diverse SPECT radioligands for the peripheral benzodiazepine receptor; Kassiou M; Australian Institute of Nuclear Science and Engineering/Awards.
  • Development and evaluation of a SPECT radioligand for imaging the sigma receptor; Kassiou M; Australian Institute of Nuclear Science and Engineering/Awards.

2003

  • Trishomocubanes: Potential neuroprotective drug therapies for Parkinsons disease; Henderson J, Kassiou M; Brain Foundation of Australia/Research Grants.
  • Development of radioligands for imaging the NMDA receptor using Positron Emission Tomography (PET); Kassiou M; Embassy of France in Australia/Research Grant.

2002

  • Not known; Kassiou M; University of Sydney (Sesqui)/Research & Development.
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Selected publications

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Book Chapters

  • Guenther, K., Hambley, T., Kassiou, M. (2008). Radiolabelled probes for imaging multidrug resistance using single photon emission tomography (SPECT) and positron emission tomography (PET). In Nicola Antonio Colabufo (Eds.), Multidrug Resistance: Biological and Pharmaceutical Advances in Antitumour Treatment, (pp. 291-320). India: Research Signpost.

Journals

  • Boutin, H., Prenant, C., Maroy, R., Galea, J., Greenhalgh, A., Smigova, A., Cawthorne, C., Julyan, P., Wilkinson, S., Banister, S., Kassiou, M., et al (2013). [(18)F]DPA-714: Direct comparison with [(11)C]PK11195 in a model of cerebral ischemia in rats. PLoS One, 8(2), e56441-1-e56441-9.
  • Wilkinson, S., Price, J., Kassiou, M. (2013). Improved accessibility to the desoxy analogues of delta(9)-tetrahydrocannabinol and cannabidiol. Tetrahedron Letters.
  • Schollhorn-Peyronneau, M., Saba, W., Goutal, S., Damont, A., Dolle, F., Kassiou, M., Bottlaender, M., Valette, H. (2013). Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligand. Drug Metabolism and Disposition, 41(1), 122-131.
  • Banister, S., Manoli, M., Kassiou, M. (2013). The development of radiotracers for imaging sigma receptors in the central nervous system (CNS) using positron emission tomography (PET). Journal of Labelled Compounds and Radiopharmaceuticals, 56(3-4), 215-224.
  • Austin, C., Kahlert, J., Kassiou, M., Rendina, L. (2013). The translocator protein (TSPO): A novel target for cancer chemotherapy. The International Journal of Biochemistry and Cell Biology, 45(7), 1212-1216.
  • Banister, S., Rendina, L., Kassiou, M. (2012). 7-azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (sigma-2) receptor ligands. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 22(12), 4059-4063.
  • Banister, S., Wilkinson, S., Hanani, R., Reynolds, A., Hibbs, D., Kassiou, M. (2012). A practical, multigram synthesis of the 2-(2-(4-alkoxyphenyl)-5,7-dimethylpy-razolo[1,5-a]pyrimidin-3-yl)acetamide (DPA) class of high affinity translocator protein (TSPO) ligands. Tetrahedron Letters, 53(29), 3780-3783.
  • Banister, S., Manoli, M., Doddareddy, M., Hibbs, D., Kassiou, M. (2012). A σ1 receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDS). Bioorganic & Medicinal Chemistry Letters, 22(19), 6053-6058.
  • Beinat, C., Banister, S., Prehn, S., Doddareddy, M., Hibbs, D., Sako, M., Collins (Chebib), M., Tran, T., Al-Muhtasib, N., Xiao, Y., Kassiou, M. (2012). Consequences of linker length alteration of the alpha7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 22(7), 2380-2384.
  • Leaver, K., Reynolds, A., Bodard, S., Guilloteau, D., Chalon, S., Kassiou, M. (2012). Effects of Translocator Protein (18 kDa) Ligands on Microglial Activation and Neuronal Death in the Quinolinic-Acid-Injected Rat Striatum. ACS Chemical Neuroscience, 3(2), 114-119.
  • Scarf, A., Luus, C., Da Pozzo, E., Selleri, S., Guarino, C., Martini, C., Ittner, L., Kassiou, M. (2012). Evidence for complex binding profiles and species differences at the translocator protein (TSPO) (18 kDa). Current Molecular Medicine, 12(4), 488-493.
  • Moussa, I., Banister, S., Manoli, M., Doddareddy, M., Cui, J., Mach, R., Kassiou, M. (2012). Exploration of ring size in a series of cyclic vicinal diamines with sigma(1) receptor-affinity. Bioorganic & Medicinal Chemistry Letters, 22(17), 5493-5497.
  • Gilmore, A., Heblinski, M., Reynolds, A., Kassiou, M., Connor, M. (2012). Inhibition of human recombinant T-type calcium channels by N-arachidonoyl 5-HT. British Journal of Pharmacology, 167(5), 1076-1088.
  • Arlicot, N., Vercouillie, J., Ribeiro, M., Tauber, C., Venel, Y., Baulieu, J., Maia, S., Corcia, P., Stabin, M., Reynolds, A., Kassiou, M., et al (2012). Initial evaluation in healthy humans of [18F]DPA-714, a potential PET biomarker for neuroinflammation. Nuclear Medicine and Biology, 39(4), 570-578.
  • Scarf, A., Aumann, K., Kassiou, M. (2012). Is there any correlation between binding and functional effects at the translocator protein (TSPO) (18 kDa)? Current Molecular Medicine, 12(4), 387-397.
  • Corcia, P., Tauber, C., Vercoullie, J., Arlicot, N., Prunier, C., Praline, J., Nicolas, G., Venel, Y., Hommet, C., Baulieu, J., Kassiou, M., et al (2012). Molecular imaging of microglial activation in amyotrophic lateral sclerosis. PLoS One, 7(12), 1-7.
  • Endres, C., Coughlin, J., Gage, K., Watkins, C., Kassiou, M., Pomper, M. (2012). Radiation dosimetry and biodistribution of the TSPO ligand (11)C-DPA-713 in humans. The Journal of Nuclear Medicine, 53(2), 330-335.
  • Gosling, J., Baker, S., Haynes, J., Kassiou, M., Pouton, C., Warfe, L., White, P., Scammells, P. (2012). Synthesis and Biological Evaluation of Adenosines with Heterobicyclic and Polycyclic N6-Substituents as Adenosine A1 Receptor Agonists. ChemMedChem: chemistry enabling drug discovery, 7(7), 1191-1201.
  • Hicks, C., Jorgensen, W., Brown, C., Fardell, J., Koehbach, J., Gruber, C., Kassiou, M., Hunt, G., McGregor, I. (2012). The Nonpeptide Oxytocin Receptor Agonist WAY 267,464: Receptor-Binding Profile, Prosocial Effects and Distribution of c-Fos Expression in Adolescent Rats. Journal of Neuroendocrinology, 24(7), 1012-1029.
  • Banister, S., Kassiou, M. (2012). The Therapeutic Potential of Sigma (sigma) Receptors for the Treatment of Central Nervous System Diseases: Evaluation of the Evidence. Current Pharmaceutical Design, 18(7), 884-901.
  • Dolle, F., Kuhnast, B., Damont, A., van Camp, N., Kassiou, M., Tavitian, B., Boisgard, R. (2011). [18F]DPA-716 as a candidate for imaging the TSPO 18 kDa with PET: Radiosynthesis and comparative evaluation ([11C]DPA-713/[18F]DPA-714) in a rat model of neuroinflammation. Journal of Labelled Compounds and Radiopharmaceuticals, 54(1), S275-S275.
  • Vercouillie, J., Ribeiro, M., Tauber, C., Venel, Y., Baulieu, J., Maia, S., Reynolds, A., Kassiou, M., Guilloteau, D., Corcia, P. (2011). Biodistribution of the TSPO radioligand (18)F-DPA-714 in healthy volunteers. Journal of Labelled Compounds and Radiopharmaceuticals, 54(1), S255-S255.
  • Issa, F., Kassiou, M., Rendina, L. (2011). Boron in drug discovery: Carboranes as unique pharmacophores in biologically active compounds. Chemical Reviews, 111(9), 5701-5722.
  • Drake, C., Boutin, H., Jones, M., Denes, A., McColl, B., Selvarajah, J., Hulme, S., Georgiou, R., Hinz, R., Gerhard, A., Kassiou, M., et al (2011). Brain inflammation is induced by co-morbidities and risk factors for stroke. Brain, Behavior, and Immunity, 25(6), 1113-1122.
  • Dolle, F., Le Helleix, S., Schollhorn-Peyronneau, M., Saba, W., Banister, S., Tournier, N., Valette, H., Kassiou, M. (2011). Carbon-11-labelling of a novel, trishomocubane-derived, high affinity and selectivity DAT ligand. Journal of Labelled Compounds and Radiopharmaceuticals, 54(1), S276-S276.
  • Moussa, I., Banister, S., Akladios, F., Chua, S., Kassiou, M. (2011). Effects of linker elongation in a series of N-(2-benzofuranylmethyl)-N'-(methoxyphenylalkyl)piperazine sigma(1) receptor ligands. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(19), 5707-5710.
  • Banister, S., Moussa, I., Jorgensen, W., Chua, S., Kassiou, M. (2011). Molecular hybridization of 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecane-3-ol with sigma (σ) receptor ligands modulates off-target activity and subtype selectivity. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(12), 3622-3626.
  • Banister, S., Yoo, D., Chua, S., Cui, J., Mach, R., Kassiou, M. (2011). N-arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (sigma) receptor ligands. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(18), 5289-5292.
  • Ribeiro, M., Vercouillie, J., Tauber, C., Venel, Y., Baulieu, J., Maia, S., Reynolds, A., Kassiou, M., Guilloteau, D., Corcia, P. (2011). P-167 The potential interest of the PET radioligand (18)F-DPA-714 in neuroinflammation. Journal of Labelled Compounds and Radiopharmaceuticals, 54(1), S256-S256.
  • Martin, A., Boisgard, R., Kassiou, M., Dolle, F., Tavitian, B. (2011). Reduced PBR/TSPO Expression After Minocycline Treatment in a Rat Model of Focal Cerebral Ischemia: A PET Study Using [(18)F]DPA-714. Molecular Imaging and Biology, 13(1), 10-15.
  • Boucher, A., Arnold, J., Hunt, G., Spiro, A., Spencer, J., Brown, C., McGregor, I., Bennett, M., Kassiou, M. (2011). Resilience and Reduced C-FOS Expression in P2X7 Receptor Knockout Mice Exposed to Repeated Forced Swim Test. Neuroscience, 189, 170-177.
  • Crossley, E., Issa, F., Scarf, A., Kassiou, M., Rendina, L. (2011). Synthesis and cellular uptake of boron-rich pyrazolopyrimidines: exploitation of the translocator protein for the efficient delivery of boron into human glioma cells. Chemical Communications, 47(44), 12179-12181.
  • Moussa, I., Banister, S., Giboureau, N., Meikle, S., Kassiou, M. (2011). Synthesis and in vivo evaluation of [18F]N-(2-benzofuranylmethyl)-N'-[4-(2-fluoroethoxy)benzyl]piperazine, a novel σ1 receptor PET imaging agent. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(22), 6820-6823.
  • Damont, A., Boisgard, R., Kuhnast, B., Lemee, F., Raggiri, G., Scarf, A., Da Pozzo, E., Selleri, S., Martini, C., Tavitian, B., Kassiou, M., et al (2011). Synthesis of 6-[(18)F]fluoro-PBR28, a novel radiotracer for imaging the TSPO 18 kDa with PET. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(16), 4819-4822.
  • Scarf, A., Kassiou, M. (2011). The translocator protein. The Journal of Nuclear Medicine, 52(5), 677-680.
  • Banister, S., Moussa, I., Beinat, C., Reynolds, A., Schiavini, P., Jorgensen, W., Kassiou, M. (2011). Trishomocubane as a Scaffold for the Development of Selective Dopamine Transporter (DAT) Ligands. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(1), 38-41.
  • Banister, S., Clegg, J., Hanani, R., Kassiou, M. (2010). 11-{[2-(3-fluorophenyl)ethyl](methyl)-amino}pentacyclo[5.4.0.0(2,6).0(3,10).0(5,9)]-undecan-8-one. Acta Crystallographica. Section E: Structure Reports Online, 66(10), o2693-o2693.
  • Naidoo (Naidoo-Variawa), S., Lehnert, W., Kassiou, M., Banati, R., Meikle, S. (2010). Attenuation correction for the large non-human primate brain imaging using microPET. Physics in Medicine and Biology, 55(8), 2351-2363.
  • Morrison, D., Issa, F., Bhadbhade, M., Groebler, L., Witting, P., Kassiou, M., Rutledge, P., Rendina, L. (2010). Boronated phosphonium salts containing arylboronic acid, closo-carborane, or nido-carborane: synthesis, X-ray diffraction, in vitro cytotoxicity, and cellular uptake. Journal of Biological Inorganic Chemistry, 15(8), 1305-1318.
  • Moussa, I., Banister, S., Beinat, C., Giboureau, N., Reynolds, A., Kassiou, M. (2010). Design, synthesis, and structure-affinity relationships of regioisomeric N-benzyl alkyl ether piperazine derivatives as sigma-1 receptor ligands. Journal of Medicinal Chemistry, 53(16), 6228-6239.
  • Giboureau, N., Aumann, K., Beinat, C., Kassiou, M. (2010). Development of vesicular acetylcholine transporter ligands: Molecular probes for Alzheimer's disease. Current Bioactive Compounds, 6(3), 129-155.
  • Abraham, M., Boisgard, R., Theze, B., Van Camp, N., Kuhnast, B., Damont, A., Kassiou, M., Dolle, F., Tavitian, B. (2010). Evaluation of the PBR/TSPO radioloigand [18F]DPA-714 in a rat model of focal cerebral ischemia. Journal of Cerebral Blood Flow and Metabolism, 30(1), 230-241.
  • Banister, S., Roeda, D., Dolle, F., Kassiou, M. (2010). Fluorine-18 chemistry for PET: A concise introduction. Current Radiopharmaceuticals, 3(2), 68-80.
  • Beinat, C., Banister, S., Moussa, I., Reynolds, A., McErlean, C., Kassiou, M. (2010). Insights into structure-activity relationships and CNS therapeutic applications of NR2B selective antagonists. Current Medicinal Chemistry, 17(34), 4166-4190.
  • Banister, S., Moussa, I., Jordan, M., Coster, M., Kassiou, M. (2010). Oxo-bridged isomers of aza-trishomocubane sigma (o) receptor ligands: Synthesis, in vitro binding, and molecular modeling. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 20(1), 145-148.
  • Gunosewoyo, H., Kassiou, M. (2010). P2X purinergic receptor ligands: Recently patented compounds. Expert Opinion on Therapeutic Patents, 20(5), 625-646.
  • Giboureau, N., Mat Som, I., Boucher, A., Guilloteau, D., Kassiou, M. (2010). PET Radioligands for the Vesicular Acetylcholine Transporter (VAChT). Current Topics in Medicinal Chemistry, 10(15), 1569-1583.
  • Reynolds, A., Hanani, R., Hibbs, D., Damont, A., Da Pozzo, E., Selleri, S., Dolle, F., Martini, C., Kassiou, M. (2010). Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO). Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 20(19), 5799-5802.
  • Luus, C., Hanani, R., Reynolds, A., Kassiou, M. (2010). The development of PET radioligands for imaging the translocator protein (18 kDa): What have we learned? Journal of Labelled Compounds and Radiopharmaceuticals, 53(7), 501-510.
  • Valette, H., Xiao, Y., Schollhorn-Peyronneau, M., Damont, A., Kosikowski, A., Wei, Z., Kassiou, M., Kellar, K., Dolle, F., Bottlaender, M. (2009). 18F-ZW-104: A New Radioligand for Imaging Neuronal Nicotinic Acetylcholine Receptors-In Vitro Binding Properties and PET Studies in Baboons. The Journal of Nuclear Medicine, 50(8), 1349-1355.
  • Doorduin, J., Klein, H., Dierckx, R., James, M., Kassiou, M., De Vries, E. (2009). [11C]-DPA-713 and [18F]-DPA-714 as new PET tracers for TSPO: A comparison with [11C]-(R)-PK11195 in a rat model of herpes encephalitis. Molecular Imaging and Biology, 11(6), 386-398.
  • Damont, A., van Camp, N., Kuhnast, B., Hinnen, F., Boisgard, R., Chauveau, F., Boutin, H., Probst, K., Clark, J., Katsifis, A., Kassiou, M. (2009). [18F]DPA-714, [18F]PBR111 and [18F]FEDAA1106 as potent PBR pet-imaging candidates: Radiosynthesis and comparative studies. Journal of Labelled Compounds and Radiopharmaceuticals, 52(S1), S122-S122.
  • Truong, L., Allbutt, H., Coster, M., Kassiou, M., Henderson, J. (2009). Behavioural effects of a selective NMDA NR1A/2B receptor antagonist in rats with unilateral 6-OHDA+ parafascicular lesions. Brain Research Bulletin, 78(2-3), 91-96.
  • Kassiou, M., Banati, R., Holsinger, R., Meikle, S. (2009). Challenges in molecular imaging of Parkinson's disease: A brief overview. Brain Research Bulletin, 78(2-3), 105-108.
  • Chauveau, F., Van Camp, N., Dolle, F., Kuhnast, B., Hinnen, F., Damont, A., Boutin, H., James, M., Kassiou, M., Tavitian, B. (2009). Comparative evaluation of the translocator protein radioligands (11)C-DPA-713, (18)F-DPA-714, and (11)C-PK11195 in a rat model of acute neuroinflammation. The Journal of Nuclear Medicine, 50(3), 468-476.
  • Warraich, S., Allbutt, H., Billing, R., Radford, J., Coster, M., Kassiou, M., Henderson, J. (2009). Evaluation of behavioural effects of a selective NMDA NR1A/2B receptor antagonist in the unilateral 6-OHDA lesion rat model. Brain Research Bulletin, 78(2-3), 85-90.
  • Edington, A., McKinzie, A., Reynolds, A., Kassiou, M., Ryan, R., Vandenberg, R. (2009). Extracellular loops 2 and 4 of GLYT2 are required for N-arachidonylglycine inhibition of glycine transport. Journal of Biological Chemistry, 284(52), 36424-36430.
  • Endres, C., Pomper, M., James, M., Uzuner, O., Hammoud, D., Watkins, C., Reynolds, A., Hilton, J., Dannals, R., Kassiou, M. (2009). Initial evaluation of 11C-DPA-713, a novel TSPO PET ligand, in humans. The Journal of Nuclear Medicine, 50(8), 1276-1282.
  • Leaver, K., Allbutt, H., Creber, N., Kassiou, M., Henderson, J. (2009). Oral pre-treatment with epigallocatechin gallate in 6-OHDA lesioned rats produces subtle symptomatic relief but not neuroprotection. Brain Research Bulletin, 80(6), 397-402.
  • Gunosewoyo, H., Coster, M., Bennett, M., Kassiou, M. (2009). Purinergic P2X(7) receptor antagonists:Chemistry and fundamentals of biological screening. Bioorganic and Medicinal Chemistry: the tetrahedron journal for research at the interface of chemistry and biology, 17(14), 4861-4865.
  • Dolle, F., Luus, C., Reynolds, A., Kassiou, M. (2009). Radiolabelled molecules for imaging the translocator protein (18 kDa) using positron emission tomography. Current Medicinal Chemistry, 16(22), 2899-2923.
  • Reynolds, A., Kassiou, M. (2009). Recent advances in the Mitsunobu reaction: Modifications and applications to biologically active molecules. Current Organic Chemistry, 13(16), 1610-1632.
  • Scarf, A., Ittner, L., Kassiou, M. (2009). The translocator protein (18 kDa): Central nervous system disease and drug design. Journal of Medicinal Chemistry, 52(3), 581-592.
  • Ioppolo, J., Kassiou, M., Rendina, L. (2009). Water-soluble phosphonium salts containing 1,12-dicarba-closo-dodecaborane(12). Tetrahedron Letters, 50(47), 6457-6461.
  • Dolle, F., Damont, A., Valette, H., Hinnen, F., Kuhnast, B., Saba, W., Schollhorn-Peyronneau, M., Kozikowski, A., Bottlaender, M., Kassiou, M. (2009). ZW-102 and ZW-104, two novel fluorine-18 labelled radioligands for imaging nicotinic acetylcholine receptors with PET. Journal of Labelled Compounds and Radiopharmaceuticals, 52(S1), S364-S364.
  • van Dijk, A., Johnston, C., Allbutt, H., Kassiou, M., Henderson, J. (2008). Behavioural effects of trishomocubanes in rats with unilateral 6-hydroxydopamine lesions. Behavioural Brain Research, 190(1), 14-21.
  • Gunosewoyo, H., Liu, G., Bennett, M., Coster, M., Kassiou, M. (2008). Cubyl amides: Novel P2X(7) receptor antagonists. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 18(13), 3720-3723.
  • Besret, L., Dolle, F., Herard, A., Guillermier, M., Demphel, S., Hinnen, F., Coulon, C., Ottaviani, M., Bottlaender, M., Hantraye, P., Kassiou, M. (2008). Dopamine D1 Receptor Imaging in the Rodent and Primate Brain Using the Isoquinoline (+)-[(11)C]A-69024 and Positron Emission Tomography. Journal of Pharmaceutical Sciences, 97(7), 2811-2819.
  • James, M., Fulton, R., Vercoullie, J., Henderson, D., Garreau, L., Chalon, S., Dolle, F., Selleri, S., Guilloteau, D., Kassiou, M. (2008). DPA-714, a New Translocator Protein-Specific Ligand: Synthesis, Radiofluorination, and Pharmacologic Characterization. The Journal of Nuclear Medicine, 49(5), 814-822.
  • Leaver, K., Allbutt, H., Creber, N., Kassiou, M., Henderson, J. (2008). Neuroprotective effects of a selective N-methyl-D-aspartate NR2B receptor antagonist in the 6-hydroxydopamine rat model of Parkinson's disease. Clinical and Experimental Pharmacology and Physiology, 35(11), 1388-1394.
  • Henderson, J., Lanciego, J., Smith, Y., Gundlach, A., Kassiou, M. (2008). Proceedings of the 2007 International Brain Research Organisation Satellite Meeting "Movement Disorders: Focus on the Thalamus and Basal Ganglia" held in Sydney, Australia, 10-11 July, 2007. Brain Research Bulletin, 78(2-3), 53-54.
  • Damont, A., Hinnen, F., Kuhnast, B., Schollhorn-Peyronneau, M., James, M., Luus, C., Tavitian, B., Kassiou, M., Dolle, F. (2008). Radiosynthesis of [(18)F]DPA-714, a selective radioligand for imaging the translocator protein (18 kDa) PET. Journal of Labelled Compounds and Radiopharmaceuticals, 51(7-8), 286-292.
  • Dolle, F., Langle, S., Roger, G., Fulton, R., Lagnel, B., Henderson, D., Hinnen, F., Paine, T., Coster, M., Valette, H., Kassiou, M., et al (2008). Synthesis and In-Vivo Evaluation of [(11)C]p-PVP-MEMA as a PET Radioligand for Imaging Nicotinic Receptors. Australian Journal of Chemistry: an international journal for chemical science, 61(6), 438-445.
  • Banister, S., Clegg, J., Coster, M., Jolliffe, K., Kassiou, M. (2007). (1R,2S,3R,6S,7R,8S)-Tricyclo[6.2.1.02,7]-undeca-4,9-diene-3,6-diol. Acta Crystallographica. Section E: Structure Reports Online, E63, o92-o93.
  • Emond, P., Mavel, S., Zea-Ponce, Y., Kassiou, M., Garreau, L., Bodard, S., Drossard, M., Chalon, S., Guilloteau, D. (2007). (E)-[125I]-5-AOIBV: a SPECT radioligand for the vesicular acetylcholine transporter. Nuclear Medicine and Biology, 34(8), 967-971.
  • Boutin, H., Chauveau, F., Thominiaux, C., Gregoire, M., James, M., Trebossen, R., Hantraye, P., Dolle, F., Tavitian, B., Kassiou, M. (2007). 11C-DPA-713: A novel peripheral benzodiazepine receptor PET ligand for in vivo imaging of neuroinflammation. The Journal of Nuclear Medicine, 48(4), 573-581.
  • Kozikowski, A., Chellappan, S., Henderson, D., Fulton, R., Giboureau, N., Xiao, Y., Wei, Z., Guilloteau, D., Emond, P., Dolle, F., Kassiou, M., et al (2007). Acetylenic pyridines for use in PET imaging of nicotinic receptors. ChemMedChem: chemistry enabling drug discovery, 2, 54-57.
  • Quinlivan, M., Chalon, S., Vergote, J., Henderson, J., Katsifis, A., Kassiou, M., Guilloteau, D. (2007). Decreased vesicular acetylcholine transporter and alpha-4beta-2 nicotinic receptor density in the rat brain following 192 IgG-saporin immunolesioning. Neuroscience Letters, 415, 97-101.
  • Giboureau, N., Emond, P., Fulton, R., Henderson, D., Chalon, S., Garreau, L., Roselt, P., Eberl, S., Mavel, S., Bodard, S., Fulham, M., Kassiou, M., et al (2007). Ex vivo and in vivo evaluation of (2R,3R)-5-[18F]-fluoroethoxy- and fluoropropoxy-benzovesamicol, as PET radioligands for the vesicular acetylcholine transporter. Synapse (New York), 61(12), 962-670.
  • Naidoo (Naidoo-Variawa), S., Hey Cunningham, A., Lehnert, W., Kench, P., Kassiou, M., Banati, R., Meikle, S. (2007). High-resolution imaging of the large non-human primate brain using microPET: a feasibility study. Physics in Medicine and Biology, 52(22), 6627-6638.
  • Collier, T., Waterhouse, R., Kassiou, M. (2007). Imaging sigma receptors: Applications in drug development. Current Pharmaceutical Design, 13, 51-72.
  • Kassiou, M. (2007). Molecular imaging in drug development (Editorial). Current Pharmaceutical Design, 13(1), 1-1.
  • Gunosewoyo, H., Coster, M., Kassiou, M. (2007). Molecular probes for P2X7 receptor studies. Current Medicinal Chemistry, 14(14), 1505-1523.
  • Cagnin, A., Kassiou, M., Meikle, S., Banati, R. (2007). Positron emission tomography imaging of neuroinflammation. Neurotherapeutics, 4(3), 443-452.
  • Liu, X., Banister, S., Christie, M., Banati, R., Meikle, S., Coster, M., Kassiou, M. (2007). Trishomocubanes: Novel sigma ligands modulate cocaine-induced behavioural effects. European Journal of Pharmacology, 555(1), 37-42.
  • Truong, L., Allbutt, H., Kassiou, M., Henderson, J. (2006). Developing a preclinical model of Parkinson's disease: a study of behaviour in rats with graded 6-OHDA lesions. Behavioural Brain Research, 169(1), 1-9.
  • James, M., Selleri, S., Kassiou, M. (2006). Development of ligands for the peripheral benzodiazepine receptor. Current Medicinal Chemistry, 13(17), 1991-2001.
  • Thominiaux, C., Dolle, F., James, M., Bramoulle, Y., Boutin, H., Besret, L., Gregoire, M., Valette, H., Bottlaender, M., Tavitian, B., Kassiou, M., et al (2006). Improved synthesis of the peripheral benzodiazepine receptor ligand C-11 DPA-713 using C-11 methyl triflate. Applied Radiation and Isotopes, 64(5), 570-573.
  • Cagnin, A., Kassiou, M., Meikle, S., Banati, R. (2006). In vivo evidence for microglial activation in neurodegenerative dementia. Acta Neurologica Scandinavica, 114(Supplement 185), 107-114.
  • Thominiaux, C., de Bruin, B., Bramoulle, Y., Hinnen, F., Demphel, S., Valette, H., Bottlaender, M., Besret, L., Kassiou, M., Dolle, F. (2006). Radiosynthesis of (E)-N-(2- C-11 methoxybenzyl)-3-phenyl-acrylamidine, a novel subnanomolar NR2B subtype-selective NMDA receptor antagonist. Applied Radiation and Isotopes, 64(3), 348-354.
  • Assaad, T., Mavel, S., Parsons, S., Kruse, S., Galineau, L., Allouchi, H., Kassiou, M., Chalon, S., Guilloteau, D., Emond, P. (2006). Synthesis and in vitro evaluation of N-substituted aza-trozamicol analogs as vesicular acetylcholine transporter ligands. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 16(10), 2654-2657.
  • Vercouillie, J., Mavel, S., Galineau, L., Ragusa, T., Innis, R., Chalon, S., Kassiou, M., Dolle, F., Besnard, J., Guilloteau, D., et al (2006). Synthesis and in vitro evaluation of novel derivatives of diphenylsulfide as serotonin transporter ligands. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 16(5), 1297-1300.
  • Issa, F., Kassiou, M., Chan, H., McLeod, M. (2006). Synthesis and radiolabelling of ipratropium and tiotropium for use as PET ligands in the study of inhaled drug deposition. Australian Journal of Chemistry: an international journal for chemical science, 59(1), 53-58.
  • Liu, X., Banister, S., Christie, M., Banati, R., Meikle, S., Coster, M., Kassiou, M. (2006). Trishomocubanes: Novel Sigma ligands modulate cocaine-induced behavioural effects. European Journal of Pharmacology, 555(1), 37-42.
  • Kassiou, M. (2005). Capabilities of PET and SPECT in pre-clinical and clinical research. Current Pharmaceutical Design, 11(25), 3201-3201.
  • Liu, X., Mattner, F., Katsifis, A., Christie, M., Kassiou, M. (2005). Influence of Trishomocubanes on Sigma Receptor Binding of N-(1-Benzylpiperidin- 4-yl)-4-[123I]iodobenzamide In Vivo in the Rat Brain. Medicinal Chemistry, 1(1), 31-38.
  • Kassiou, M., Meikle, S., Banati, R. (2005). Ligands for peripheral benzodiazepine binding sites in glial cells. Brain Research Reviews, 48(2), 207-210.
  • Mohamed, A., Eberl, S., Fulham, M., Kassiou, M., Zaman, A., Henderson, D., Beveridge, S., Constable, C., Lo, S. (2005). Sequential 123I-iododexetimide scans in temporal lobe epilepsy: comparison with neuroimaging scans (MR imaging and F-18-FDG PET imaging). European Journal of Nuclear Medicine and Molecular Imaging, 32(2), 180-185.
  • Meikle, S., Kench, P., Kassiou, M., Banati, R. (2005). Small animal SPECT and its place in the matrix of molecular imaging technologies. Physics in Medicine and Biology, 50(22), R45-R61.
  • Zea-Ponce, Y., Mavel, S., Assaad, T., Kruse, S., Parsons, S., Emond, P., Chalon, S., Giboureau, N., Kassiou, M., Guilloteau, D. (2005). Synthesis and in vitro evaluation of new benzovesamicol analogues as potential imaging probes for the vesicular acetylcholine transporter. Bioorganic and Medicinal Chemistry: the tetrahedron journal for research at the interface of chemistry and biology, 13(3), 745-753.
  • Kassiou, M., Dannals, R., Liu, X., Wong, D., Ravert, H., Scheffel, U. (2005). Synthesis and in vivo evaluation of a new PET radioligand for studying sigma-2 receptors. Bioorganic and Medicinal Chemistry: the tetrahedron journal for research at the interface of chemistry and biology, 13(11), 3623-3626.
  • James, M., Fulton, R., Henderson, D., Eberl, S., Meikle, S., Thomson, S., Allan, R., Dolle, F., Fulham, M., Kassiou, M. (2005). Synthesis and in vivo evaluation of a novel peripheral benzodiazepine receptor PET radioligand. Bioorganic and Medicinal Chemistry: the tetrahedron journal for research at the interface of chemistry and biology, 13(22), 6188-6194.
  • Henderson, D., Eberl, S., Thomson, S., Smith, A., Allan, R., Fulham, M., Loiacono, R., Kassiou, M. (2004). 3-Pyridyl Ethers As Spect Radioligands For Imaging Nicotinic Acetylcholine Receptors. Applied Radiation and Isotopes, 60(5), 669-676.
  • Katsifis, A., Kassiou, M. (2004). Development Of Radioligands For In Vivo Imaging Of Gaba(A)-Benzodiazepine Receptors. Mini - Reviews in Medicinal Chemistry, 4(8), 909-921.
  • Dolle, F., Valette, H., Demphel, S., Coulon, C., Ottaviani, M., Bottlaender, M., Kassiou, M. (2004). Radiosynthesis And In Vivo Evaluation Of [11C]Ro-547312: A Novel Nr1/2B Subtype Selective Nmda Receptor Radioligand. Journal of Labelled Compounds and Radiopharmaceuticals, 47(13), 911-920.
  • Roger, G., Dolle, F., de Bruin, B., Liu, X., Besret, L., Bramoulle, Y., Coulon, C., Ottaviani, M., Bottlaender, M., Valette, H., Kassiou, M. (2004). Radiosynthesis And Pharmacological Evaluation Of [11C]Emd-95885: A High Affinity Ligand For Nr2B-Containing Nmda Receptors. Bioorganic and Medicinal Chemistry: the tetrahedron journal for research at the interface of chemistry and biology, 12(12), 3229-3237.
  • Roselt, P., Meikle, S., Kassiou, M. (2004). The Role Of Positron Emission Tomography In The Discovery And Development Of New Drugs; As Studied In Laboratory Animals. European Journal of Drug Metabolism and Pharmacokinetics, 29(1), 1-6.
  • Kassiou, M., Katsifis, A. (2003). PET radiochemistry in drug development and evaluation. Chemistry in Australia, 70(5), 10-12.
  • Katsifis, A., Mardon, K., Mattner, F., Loc'h, C., McPhee, M., Dikic, B., Kassiou, M., Ridley, D. (2003). Pharmacological evaluation of (S)-8-[123I]iodobretazenil: a radioligand for in vivo studies of central benzodiazepine receptors. Nuclear Medicine and Biology, 30(2), 191-198.
  • Quinlivan, M., Mattner, F., Papazian, V., Zhou, J., Katsifis, A., Emond, P., Chalon, S., Kozikowski, A., Guilloteau, D., Kassiou, M. (2003). Synthesis and evaluation of iodine-123 labelled tricyclic tropanes as radioligands for the serotonin transporter. Nuclear Medicine and Biology, 30(7), 741-746.
  • Roger, G., Lagnel, B., Besret, L., Bramoulle, Y., Coulon, C., Ottaviani, M., Kassiou, M., Bottlaender, M., Valette, H., Dolle, F. (2003). Synthesis, radiosynthesis and In Vivo evaluation of 5-[3-(4-Benzylpiperidin-1-yl) prop-1-ynyl]-1, 3-dihydrobenzoimidazol-2-[11C] one, as a potent NR 1A/2B subtype selective NMDA PET radiotracer. Bioorganic and Medicinal Chemistry: the tetrahedron journal for research at the interface of chemistry and biology, 11, 5401-5408.
  • Kassiou, M., Loc'h, C., Bottlaender, M., Mardon, K., Ottaviani, M., Coulon, C., Katsifis, A., Maziere, B. (2002). (+)-[76Br]A-69024: a non-benzazepine radioligand for studies of dopamine D1 receptors using PET. Nuclear Medicine and Biology, 29(3), 295-302.
  • Kassiou, M., Bottlaender, M., Loc'h, C., Dolle, F., Musachio, J., Coulon, C., Ottaviani, M., Dannals, R., Maziere, B. (2002). Pharmacological evaluation of a Br-76 analog of epibatidine: a potent ligand for studying brain nicotinic acetylcholine receptors. Synapse (New York), 45(2), 95-104.
  • Kassiou, M., Loc'h, C., Dolle, F., Musachio, J., Dolci, L., Crouzel, C., Dannals, R., Maziere, B. (2002). Preparation of a bromine-76 labelled analogue of epibatidine: a potent ligand for nicotinic acetylcholine receptor studies. Applied Radiation and Isotopes, 57(5), 713-717.
  • Kassiou, M., Eberl, S., Meikle, S., Birrell, A., Constable, C., Fulham, M., Wong, D., Musachio, J. (2001). In vivo imaging of nicotinic receptor upregulation following chronic (-)-nicotine treatment in baboon using SPECT. Nuclear Medicine and Biology, 28, 165-175.
  • Kassiou, M., Mardon, K., Mattner,, F., Katsifis, A., Dikic, B. (2001). Pharmacological evaluation of (+)-2-[123I]A-69024: A radioligand for in vivo studies of dopamine D1 receptors. Life Sciences, 69, 669-675.
  • Liu, X., Christie, M., Kassiou, M., Nuwayhid, S., Werling, L. (2001). Trishomocubanes: Novel sigma-ligands modulate amphetamine-stimulated [3H]dopamine release. European Journal of Pharmacology, 422, 39-45.
  • Liu, X., Kassiou, M., Christie, M., Hambley, T. (2001). Trishomocubanes: requirements for sigma receptor binding and subtype selectivity. Australian Journal of Chemistry: an international journal for chemical science, 54, 31-36.

Conferences

  • Fulham, M., Kassiou, M., Greguric, I., Thomson, S., Eberl, S., Tiam, P., Mattner, F., Henderson, D., Fulton, R., Katsifis, A., et al (2012). Synthesis and in vivo evaluation of arylalkyl 4-benzyl piperidines as radioligands for sigma receptors. 16th International Symposium on Radiopharmaceutical Chemistry, United Kingdom: Wiley.
  • Fulton, R., Meikle, S., Kyme, A., Zhou, W., Popovic, K., Kassiou, M., Akhtar, M. (2010). Motion-corrected microPET brain imaging of conscious rats. 2009 World Molecular Imaging Conference, USB drive/online: Online.
  • Banister, S., Coster, M., Kassiou, M. (2009). A versatile polycyclic scaffold for the discovery of selective sigma (sigma) receptor ligands (POSTER/TALK). 7th AFMC International Medicinal Chemistry Symposium, N/A: N/A.
  • Kassiou, M. (2009). Discovery of new therapeutic immunomodulator drugs as a pathway for treating brain disease (POSTER/TALK). Plant Nutraceuticals and Bioactive Molecules: A Growth Opportunity for the Pharmaceutical Industry in Australia and India, N/A: N/A.
  • Kassiou, M. (2009). Imaging immune response in the CNS - Applications for therapeutic development (POSTER/TALK). 7th AFMC International Medicinal Chemistry Symposium, N/A: N/A.
  • Moussa, I., Coster, M., Kassiou, M. (2009). Synthesis and pharmacological evaluation of novel sigma receptor ligands (POSTER/TALK). 7th AFMC International Medicinal Chemistry Symposium, N/A: N/A.
  • Fulton, R., Kyme, A., Zhou, V., Leaver, K., Kassiou, M., Lehnert, W., Meikle, S. (2008). Progress towards microPET imaging of small, awake laboratory animals. 2008 World Molecular Imaging Congress, Europe: World Molecular Imaging Congress.
  • Doorduin, J., Klein, H., James, M., Kassiou, M., Dierckx, R., Vries, E. (2007). (18F)DPA-714 as a novel PET tracer for PBR: A comparison with (11C)PK11195 in a rat model of HSV encephalitis. 17th International Symposium on Radiopharmaceutical Sciences. John Wiley & Sons.
  • James, M., Fulton, R., Vercouille, J., Henderson, D., Garreau, L., Eberl, S., Chalon, S., Selleri, S., Dolle, F., Guilloteau, D., Kassiou, M. (2007). DPA-714 A new translocator protein (18kDa) ligand: Synthesis, radiofluorination and pharmacological characterisation. 17th International Symposium on Radiopharmaceutical Sciences. John Wiley & Sons.
  • Mavel, S., Zea-Ponce, Y., Garreau, L., Chalon, S., Kassiou, M., Guilloteau, D., Emond, P. (2007). E-((R,R) and (S,S))-5-(125I)-AOIBV: Potential SPECT tracers in vivo studies of the vesicular AcetylCholine Transporter (VACht). 17th International Symposium on Radiopharmaceutical Sciences. John Wiley & Sons.
  • Kassiou, M., Chellappan, S., Henderson, D., Fulton, R., Giboureau, N., Xiao, Y., Wei, Z., Guilloteau, D., Emond, P., Dolle, F., et al (2007). Radiosynthesis and preliminary evaluation of ZW-90 and ZW-110, two novel acetylenic pyridines for imaging nicotonic receptors. 17th International Symposium on Radiopharmaceutical Sciences. John Wiley & Sons.
  • Giboureau, N., Chalon, S., Garreau, L., Kassiou, M., Emond, P., Guilloteau, D. (2007). Rat distribution of (18F)-Fuoropropoxy- and (18F)-Fluoroethoxybenzovesamicol, as PET radioligands for the vesicular acetylcholine transporter (VACht). 17th International Symposium on Radiopharmaceutical Sciences. John Wiley & Sons.
  • Creelman, A., Thominiaux, C., Chauveau, F., Fulton, R., Kuhnast, B., Henderson, D., Boutin, H., Selleri, S., McGregor, I., Hantraye, P., Kassiou, M., et al (2007). Synthesis and evaluation of the translocator protein (18kDa) (TSPO) ligand (11C)DPA0715 in rat and non-human primate. 17th International Symposium on Radiopharmaceutical Sciences. John Wiley & Sons.
  • Langley, S., Roger, G., Fulton, R., Lagnel, B., Henderson, D., Hinnen, F., Bottlaender, M., Dolle, F., Kassiou, M. (2007). Synthesis and in vivo evaluation of (11c)P-PVP-MEMA as a PET radioligand for Imaging nicotonic receptors. 17th International Symposium on Radiopharmaceutical Sciences. John Wiley & Sons.
  • Kassiou, M., Bruin, B., Demphel, S., Besret, L., Hinnen, F., Dolle, F., Bramoulle, Y., Thominiaux, C., Bottlaender, M. (2005). Radiosynthesis of (E)-N-(2-[11C]methoxybenzyl)-3-phenyl-acrylamidine, a novel subnanomolar NR2B subtype-selective NMDA receptor ligand. 16th International Symposium on Radiopharmaceutical Chemistry, United Kingdom: Wiley.
  • Fulham, M., Kassiou, M., Dolle, F., Thomson, S., Henderson, D., James, M., Eberl, S., Fulton, R., Allan, R. (2005). Synthesis and In Vivo Evaluation of a Novel Peripheral Benzodiazepine Receptor PET Radioligand. 16th International Symposium on Radiopharmaceutical Chemistry, United Kingdom: Wiley.
  • Feng, D., Kassiou, M., Fulham, M., Wong, K., Elberl, S. (2003). Quantification of 5-[123I]iodo-A-85380 in nonhuman primates using spect: parameter identifiability and stabilitty. Modelling and Control in Biomedical Systems 2003 (Including Biological Systems), UK: Pergamon.

Patents

  • Kassiou, M., James, M. (2010). 2-Arylpyrazolo[L,5-a]Pyrimidin-3-yl Acetamide Deriv As Ligands For Translocator Protein. Patent No. 2008/10473. South Africa.
  • Kassiou, M., James, M., Luus, C. (2009). Patent No. WO2009079683 (A1).

2013

  • Boutin, H., Prenant, C., Maroy, R., Galea, J., Greenhalgh, A., Smigova, A., Cawthorne, C., Julyan, P., Wilkinson, S., Banister, S., Kassiou, M., et al (2013). [(18)F]DPA-714: Direct comparison with [(11)C]PK11195 in a model of cerebral ischemia in rats. PLoS One, 8(2), e56441-1-e56441-9.
  • Wilkinson, S., Price, J., Kassiou, M. (2013). Improved accessibility to the desoxy analogues of delta(9)-tetrahydrocannabinol and cannabidiol. Tetrahedron Letters.
  • Schollhorn-Peyronneau, M., Saba, W., Goutal, S., Damont, A., Dolle, F., Kassiou, M., Bottlaender, M., Valette, H. (2013). Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligand. Drug Metabolism and Disposition, 41(1), 122-131.
  • Banister, S., Manoli, M., Kassiou, M. (2013). The development of radiotracers for imaging sigma receptors in the central nervous system (CNS) using positron emission tomography (PET). Journal of Labelled Compounds and Radiopharmaceuticals, 56(3-4), 215-224.
  • Austin, C., Kahlert, J., Kassiou, M., Rendina, L. (2013). The translocator protein (TSPO): A novel target for cancer chemotherapy. The International Journal of Biochemistry and Cell Biology, 45(7), 1212-1216.

2012

  • Banister, S., Rendina, L., Kassiou, M. (2012). 7-azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (sigma-2) receptor ligands. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 22(12), 4059-4063.
  • Banister, S., Wilkinson, S., Hanani, R., Reynolds, A., Hibbs, D., Kassiou, M. (2012). A practical, multigram synthesis of the 2-(2-(4-alkoxyphenyl)-5,7-dimethylpy-razolo[1,5-a]pyrimidin-3-yl)acetamide (DPA) class of high affinity translocator protein (TSPO) ligands. Tetrahedron Letters, 53(29), 3780-3783.
  • Banister, S., Manoli, M., Doddareddy, M., Hibbs, D., Kassiou, M. (2012). A σ1 receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDS). Bioorganic & Medicinal Chemistry Letters, 22(19), 6053-6058.
  • Beinat, C., Banister, S., Prehn, S., Doddareddy, M., Hibbs, D., Sako, M., Collins (Chebib), M., Tran, T., Al-Muhtasib, N., Xiao, Y., Kassiou, M. (2012). Consequences of linker length alteration of the alpha7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 22(7), 2380-2384.
  • Leaver, K., Reynolds, A., Bodard, S., Guilloteau, D., Chalon, S., Kassiou, M. (2012). Effects of Translocator Protein (18 kDa) Ligands on Microglial Activation and Neuronal Death in the Quinolinic-Acid-Injected Rat Striatum. ACS Chemical Neuroscience, 3(2), 114-119.
  • Scarf, A., Luus, C., Da Pozzo, E., Selleri, S., Guarino, C., Martini, C., Ittner, L., Kassiou, M. (2012). Evidence for complex binding profiles and species differences at the translocator protein (TSPO) (18 kDa). Current Molecular Medicine, 12(4), 488-493.
  • Moussa, I., Banister, S., Manoli, M., Doddareddy, M., Cui, J., Mach, R., Kassiou, M. (2012). Exploration of ring size in a series of cyclic vicinal diamines with sigma(1) receptor-affinity. Bioorganic & Medicinal Chemistry Letters, 22(17), 5493-5497.
  • Gilmore, A., Heblinski, M., Reynolds, A., Kassiou, M., Connor, M. (2012). Inhibition of human recombinant T-type calcium channels by N-arachidonoyl 5-HT. British Journal of Pharmacology, 167(5), 1076-1088.
  • Arlicot, N., Vercouillie, J., Ribeiro, M., Tauber, C., Venel, Y., Baulieu, J., Maia, S., Corcia, P., Stabin, M., Reynolds, A., Kassiou, M., et al (2012). Initial evaluation in healthy humans of [18F]DPA-714, a potential PET biomarker for neuroinflammation. Nuclear Medicine and Biology, 39(4), 570-578.
  • Scarf, A., Aumann, K., Kassiou, M. (2012). Is there any correlation between binding and functional effects at the translocator protein (TSPO) (18 kDa)? Current Molecular Medicine, 12(4), 387-397.
  • Corcia, P., Tauber, C., Vercoullie, J., Arlicot, N., Prunier, C., Praline, J., Nicolas, G., Venel, Y., Hommet, C., Baulieu, J., Kassiou, M., et al (2012). Molecular imaging of microglial activation in amyotrophic lateral sclerosis. PLoS One, 7(12), 1-7.
  • Endres, C., Coughlin, J., Gage, K., Watkins, C., Kassiou, M., Pomper, M. (2012). Radiation dosimetry and biodistribution of the TSPO ligand (11)C-DPA-713 in humans. The Journal of Nuclear Medicine, 53(2), 330-335.
  • Gosling, J., Baker, S., Haynes, J., Kassiou, M., Pouton, C., Warfe, L., White, P., Scammells, P. (2012). Synthesis and Biological Evaluation of Adenosines with Heterobicyclic and Polycyclic N6-Substituents as Adenosine A1 Receptor Agonists. ChemMedChem: chemistry enabling drug discovery, 7(7), 1191-1201.
  • Fulham, M., Kassiou, M., Greguric, I., Thomson, S., Eberl, S., Tiam, P., Mattner, F., Henderson, D., Fulton, R., Katsifis, A., et al (2012). Synthesis and in vivo evaluation of arylalkyl 4-benzyl piperidines as radioligands for sigma receptors. 16th International Symposium on Radiopharmaceutical Chemistry, United Kingdom: Wiley.
  • Hicks, C., Jorgensen, W., Brown, C., Fardell, J., Koehbach, J., Gruber, C., Kassiou, M., Hunt, G., McGregor, I. (2012). The Nonpeptide Oxytocin Receptor Agonist WAY 267,464: Receptor-Binding Profile, Prosocial Effects and Distribution of c-Fos Expression in Adolescent Rats. Journal of Neuroendocrinology, 24(7), 1012-1029.
  • Banister, S., Kassiou, M. (2012). The Therapeutic Potential of Sigma (sigma) Receptors for the Treatment of Central Nervous System Diseases: Evaluation of the Evidence. Current Pharmaceutical Design, 18(7), 884-901.

2011

  • Dolle, F., Kuhnast, B., Damont, A., van Camp, N., Kassiou, M., Tavitian, B., Boisgard, R. (2011). [18F]DPA-716 as a candidate for imaging the TSPO 18 kDa with PET: Radiosynthesis and comparative evaluation ([11C]DPA-713/[18F]DPA-714) in a rat model of neuroinflammation. Journal of Labelled Compounds and Radiopharmaceuticals, 54(1), S275-S275.
  • Vercouillie, J., Ribeiro, M., Tauber, C., Venel, Y., Baulieu, J., Maia, S., Reynolds, A., Kassiou, M., Guilloteau, D., Corcia, P. (2011). Biodistribution of the TSPO radioligand (18)F-DPA-714 in healthy volunteers. Journal of Labelled Compounds and Radiopharmaceuticals, 54(1), S255-S255.
  • Issa, F., Kassiou, M., Rendina, L. (2011). Boron in drug discovery: Carboranes as unique pharmacophores in biologically active compounds. Chemical Reviews, 111(9), 5701-5722.
  • Drake, C., Boutin, H., Jones, M., Denes, A., McColl, B., Selvarajah, J., Hulme, S., Georgiou, R., Hinz, R., Gerhard, A., Kassiou, M., et al (2011). Brain inflammation is induced by co-morbidities and risk factors for stroke. Brain, Behavior, and Immunity, 25(6), 1113-1122.
  • Dolle, F., Le Helleix, S., Schollhorn-Peyronneau, M., Saba, W., Banister, S., Tournier, N., Valette, H., Kassiou, M. (2011). Carbon-11-labelling of a novel, trishomocubane-derived, high affinity and selectivity DAT ligand. Journal of Labelled Compounds and Radiopharmaceuticals, 54(1), S276-S276.
  • Moussa, I., Banister, S., Akladios, F., Chua, S., Kassiou, M. (2011). Effects of linker elongation in a series of N-(2-benzofuranylmethyl)-N'-(methoxyphenylalkyl)piperazine sigma(1) receptor ligands. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(19), 5707-5710.
  • Banister, S., Moussa, I., Jorgensen, W., Chua, S., Kassiou, M. (2011). Molecular hybridization of 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecane-3-ol with sigma (σ) receptor ligands modulates off-target activity and subtype selectivity. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(12), 3622-3626.
  • Banister, S., Yoo, D., Chua, S., Cui, J., Mach, R., Kassiou, M. (2011). N-arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (sigma) receptor ligands. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(18), 5289-5292.
  • Ribeiro, M., Vercouillie, J., Tauber, C., Venel, Y., Baulieu, J., Maia, S., Reynolds, A., Kassiou, M., Guilloteau, D., Corcia, P. (2011). P-167 The potential interest of the PET radioligand (18)F-DPA-714 in neuroinflammation. Journal of Labelled Compounds and Radiopharmaceuticals, 54(1), S256-S256.
  • Martin, A., Boisgard, R., Kassiou, M., Dolle, F., Tavitian, B. (2011). Reduced PBR/TSPO Expression After Minocycline Treatment in a Rat Model of Focal Cerebral Ischemia: A PET Study Using [(18)F]DPA-714. Molecular Imaging and Biology, 13(1), 10-15.
  • Boucher, A., Arnold, J., Hunt, G., Spiro, A., Spencer, J., Brown, C., McGregor, I., Bennett, M., Kassiou, M. (2011). Resilience and Reduced C-FOS Expression in P2X7 Receptor Knockout Mice Exposed to Repeated Forced Swim Test. Neuroscience, 189, 170-177.
  • Crossley, E., Issa, F., Scarf, A., Kassiou, M., Rendina, L. (2011). Synthesis and cellular uptake of boron-rich pyrazolopyrimidines: exploitation of the translocator protein for the efficient delivery of boron into human glioma cells. Chemical Communications, 47(44), 12179-12181.
  • Moussa, I., Banister, S., Giboureau, N., Meikle, S., Kassiou, M. (2011). Synthesis and in vivo evaluation of [18F]N-(2-benzofuranylmethyl)-N'-[4-(2-fluoroethoxy)benzyl]piperazine, a novel σ1 receptor PET imaging agent. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(22), 6820-6823.
  • Damont, A., Boisgard, R., Kuhnast, B., Lemee, F., Raggiri, G., Scarf, A., Da Pozzo, E., Selleri, S., Martini, C., Tavitian, B., Kassiou, M., et al (2011). Synthesis of 6-[(18)F]fluoro-PBR28, a novel radiotracer for imaging the TSPO 18 kDa with PET. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(16), 4819-4822.
  • Scarf, A., Kassiou, M. (2011). The translocator protein. The Journal of Nuclear Medicine, 52(5), 677-680.
  • Banister, S., Moussa, I., Beinat, C., Reynolds, A., Schiavini, P., Jorgensen, W., Kassiou, M. (2011). Trishomocubane as a Scaffold for the Development of Selective Dopamine Transporter (DAT) Ligands. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(1), 38-41.

2010

  • Banister, S., Clegg, J., Hanani, R., Kassiou, M. (2010). 11-{[2-(3-fluorophenyl)ethyl](methyl)-amino}pentacyclo[5.4.0.0(2,6).0(3,10).0(5,9)]-undecan-8-one. Acta Crystallographica. Section E: Structure Reports Online, 66(10), o2693-o2693.
  • Kassiou, M., James, M. (2010). 2-Arylpyrazolo[L,5-a]Pyrimidin-3-yl Acetamide Deriv As Ligands For Translocator Protein. Patent No. 2008/10473. South Africa.
  • Naidoo (Naidoo-Variawa), S., Lehnert, W., Kassiou, M., Banati, R., Meikle, S. (2010). Attenuation correction for the large non-human primate brain imaging using microPET. Physics in Medicine and Biology, 55(8), 2351-2363.
  • Morrison, D., Issa, F., Bhadbhade, M., Groebler, L., Witting, P., Kassiou, M., Rutledge, P., Rendina, L. (2010). Boronated phosphonium salts containing arylboronic acid, closo-carborane, or nido-carborane: synthesis, X-ray diffraction, in vitro cytotoxicity, and cellular uptake. Journal of Biological Inorganic Chemistry, 15(8), 1305-1318.
  • Moussa, I., Banister, S., Beinat, C., Giboureau, N., Reynolds, A., Kassiou, M. (2010). Design, synthesis, and structure-affinity relationships of regioisomeric N-benzyl alkyl ether piperazine derivatives as sigma-1 receptor ligands. Journal of Medicinal Chemistry, 53(16), 6228-6239.
  • Giboureau, N., Aumann, K., Beinat, C., Kassiou, M. (2010). Development of vesicular acetylcholine transporter ligands: Molecular probes for Alzheimer's disease. Current Bioactive Compounds, 6(3), 129-155.
  • Abraham, M., Boisgard, R., Theze, B., Van Camp, N., Kuhnast, B., Damont, A., Kassiou, M., Dolle, F., Tavitian, B. (2010). Evaluation of the PBR/TSPO radioloigand [18F]DPA-714 in a rat model of focal cerebral ischemia. Journal of Cerebral Blood Flow and Metabolism, 30(1), 230-241.
  • Banister, S., Roeda, D., Dolle, F., Kassiou, M. (2010). Fluorine-18 chemistry for PET: A concise introduction. Current Radiopharmaceuticals, 3(2), 68-80.
  • Beinat, C., Banister, S., Moussa, I., Reynolds, A., McErlean, C., Kassiou, M. (2010). Insights into structure-activity relationships and CNS therapeutic applications of NR2B selective antagonists. Current Medicinal Chemistry, 17(34), 4166-4190.
  • Fulton, R., Meikle, S., Kyme, A., Zhou, W., Popovic, K., Kassiou, M., Akhtar, M. (2010). Motion-corrected microPET brain imaging of conscious rats. 2009 World Molecular Imaging Conference, USB drive/online: Online.
  • Banister, S., Moussa, I., Jordan, M., Coster, M., Kassiou, M. (2010). Oxo-bridged isomers of aza-trishomocubane sigma (o) receptor ligands: Synthesis, in vitro binding, and molecular modeling. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 20(1), 145-148.
  • Gunosewoyo, H., Kassiou, M. (2010). P2X purinergic receptor ligands: Recently patented compounds. Expert Opinion on Therapeutic Patents, 20(5), 625-646.
  • Giboureau, N., Mat Som, I., Boucher, A., Guilloteau, D., Kassiou, M. (2010). PET Radioligands for the Vesicular Acetylcholine Transporter (VAChT). Current Topics in Medicinal Chemistry, 10(15), 1569-1583.
  • Reynolds, A., Hanani, R., Hibbs, D., Damont, A., Da Pozzo, E., Selleri, S., Dolle, F., Martini, C., Kassiou, M. (2010). Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO). Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 20(19), 5799-5802.
  • Luus, C., Hanani, R., Reynolds, A., Kassiou, M. (2010). The development of PET radioligands for imaging the translocator protein (18 kDa): What have we learned? Journal of Labelled Compounds and Radiopharmaceuticals, 53(7), 501-510.

2009

  • Valette, H., Xiao, Y., Schollhorn-Peyronneau, M., Damont, A., Kosikowski, A., Wei, Z., Kassiou, M., Kellar, K., Dolle, F., Bottlaender, M. (2009). 18F-ZW-104: A New Radioligand for Imaging Neuronal Nicotinic Acetylcholine Receptors-In Vitro Binding Properties and PET Studies in Baboons. The Journal of Nuclear Medicine, 50(8), 1349-1355.
  • Doorduin, J., Klein, H., Dierckx, R., James, M., Kassiou, M., De Vries, E. (2009). [11C]-DPA-713 and [18F]-DPA-714 as new PET tracers for TSPO: A comparison with [11C]-(R)-PK11195 in a rat model of herpes encephalitis. Molecular Imaging and Biology, 11(6), 386-398.
  • Damont, A., van Camp, N., Kuhnast, B., Hinnen, F., Boisgard, R., Chauveau, F., Boutin, H., Probst, K., Clark, J., Katsifis, A., Kassiou, M. (2009). [18F]DPA-714, [18F]PBR111 and [18F]FEDAA1106 as potent PBR pet-imaging candidates: Radiosynthesis and comparative studies. Journal of Labelled Compounds and Radiopharmaceuticals, 52(S1), S122-S122.
  • Banister, S., Coster, M., Kassiou, M. (2009). A versatile polycyclic scaffold for the discovery of selective sigma (sigma) receptor ligands (POSTER/TALK). 7th AFMC International Medicinal Chemistry Symposium, N/A: N/A.
  • Truong, L., Allbutt, H., Coster, M., Kassiou, M., Henderson, J. (2009). Behavioural effects of a selective NMDA NR1A/2B receptor antagonist in rats with unilateral 6-OHDA+ parafascicular lesions. Brain Research Bulletin, 78(2-3), 91-96.
  • Kassiou, M., Banati, R., Holsinger, R., Meikle, S. (2009). Challenges in molecular imaging of Parkinson's disease: A brief overview. Brain Research Bulletin, 78(2-3), 105-108.
  • Chauveau, F., Van Camp, N., Dolle, F., Kuhnast, B., Hinnen, F., Damont, A., Boutin, H., James, M., Kassiou, M., Tavitian, B. (2009). Comparative evaluation of the translocator protein radioligands (11)C-DPA-713, (18)F-DPA-714, and (11)C-PK11195 in a rat model of acute neuroinflammation. The Journal of Nuclear Medicine, 50(3), 468-476.
  • Kassiou, M. (2009). Discovery of new therapeutic immunomodulator drugs as a pathway for treating brain disease (POSTER/TALK). Plant Nutraceuticals and Bioactive Molecules: A Growth Opportunity for the Pharmaceutical Industry in Australia and India, N/A: N/A.
  • Warraich, S., Allbutt, H., Billing, R., Radford, J., Coster, M., Kassiou, M., Henderson, J. (2009). Evaluation of behavioural effects of a selective NMDA NR1A/2B receptor antagonist in the unilateral 6-OHDA lesion rat model. Brain Research Bulletin, 78(2-3), 85-90.
  • Edington, A., McKinzie, A., Reynolds, A., Kassiou, M., Ryan, R., Vandenberg, R. (2009). Extracellular loops 2 and 4 of GLYT2 are required for N-arachidonylglycine inhibition of glycine transport. Journal of Biological Chemistry, 284(52), 36424-36430.
  • Kassiou, M. (2009). Imaging immune response in the CNS - Applications for therapeutic development (POSTER/TALK). 7th AFMC International Medicinal Chemistry Symposium, N/A: N/A.
  • Endres, C., Pomper, M., James, M., Uzuner, O., Hammoud, D., Watkins, C., Reynolds, A., Hilton, J., Dannals, R., Kassiou, M. (2009). Initial evaluation of 11C-DPA-713, a novel TSPO PET ligand, in humans. The Journal of Nuclear Medicine, 50(8), 1276-1282.
  • Leaver, K., Allbutt, H., Creber, N., Kassiou, M., Henderson, J. (2009). Oral pre-treatment with epigallocatechin gallate in 6-OHDA lesioned rats produces subtle symptomatic relief but not neuroprotection. Brain Research Bulletin, 80(6), 397-402.
  • Kassiou, M., James, M., Luus, C. (2009). Patent No. WO2009079683 (A1).
  • Gunosewoyo, H., Coster, M., Bennett, M., Kassiou, M. (2009). Purinergic P2X(7) receptor antagonists:Chemistry and fundamentals of biological screening. Bioorganic and Medicinal Chemistry: the tetrahedron journal for research at the interface of chemistry and biology, 17(14), 4861-4865.
  • Dolle, F., Luus, C., Reynolds, A., Kassiou, M. (2009). Radiolabelled molecules for imaging the translocator protein (18 kDa) using positron emission tomography. Current Medicinal Chemistry, 16(22), 2899-2923.
  • Reynolds, A., Kassiou, M. (2009). Recent advances in the Mitsunobu reaction: Modifications and applications to biologically active molecules. Current Organic Chemistry, 13(16), 1610-1632.
  • Moussa, I., Coster, M., Kassiou, M. (2009). Synthesis and pharmacological evaluation of novel sigma receptor ligands (POSTER/TALK). 7th AFMC International Medicinal Chemistry Symposium, N/A: N/A.
  • Scarf, A., Ittner, L., Kassiou, M. (2009). The translocator protein (18 kDa): Central nervous system disease and drug design. Journal of Medicinal Chemistry, 52(3), 581-592.
  • Ioppolo, J., Kassiou, M., Rendina, L. (2009). Water-soluble phosphonium salts containing 1,12-dicarba-closo-dodecaborane(12). Tetrahedron Letters, 50(47), 6457-6461.
  • Dolle, F., Damont, A., Valette, H., Hinnen, F., Kuhnast, B., Saba, W., Schollhorn-Peyronneau, M., Kozikowski, A., Bottlaender, M., Kassiou, M. (2009). ZW-102 and ZW-104, two novel fluorine-18 labelled radioligands for imaging nicotinic acetylcholine receptors with PET. Journal of Labelled Compounds and Radiopharmaceuticals, 52(S1), S364-S364.

2008

  • van Dijk, A., Johnston, C., Allbutt, H., Kassiou, M., Henderson, J. (2008). Behavioural effects of trishomocubanes in rats with unilateral 6-hydroxydopamine lesions. Behavioural Brain Research, 190(1), 14-21.
  • Gunosewoyo, H., Liu, G., Bennett, M., Coster, M., Kassiou, M. (2008). Cubyl amides: Novel P2X(7) receptor antagonists. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 18(13), 3720-3723.
  • Besret, L., Dolle, F., Herard, A., Guillermier, M., Demphel, S., Hinnen, F., Coulon, C., Ottaviani, M., Bottlaender, M., Hantraye, P., Kassiou, M. (2008). Dopamine D1 Receptor Imaging in the Rodent and Primate Brain Using the Isoquinoline (+)-[(11)C]A-69024 and Positron Emission Tomography. Journal of Pharmaceutical Sciences, 97(7), 2811-2819.
  • James, M., Fulton, R., Vercoullie, J., Henderson, D., Garreau, L., Chalon, S., Dolle, F., Selleri, S., Guilloteau, D., Kassiou, M. (2008). DPA-714, a New Translocator Protein-Specific Ligand: Synthesis, Radiofluorination, and Pharmacologic Characterization. The Journal of Nuclear Medicine, 49(5), 814-822.
  • Leaver, K., Allbutt, H., Creber, N., Kassiou, M., Henderson, J. (2008). Neuroprotective effects of a selective N-methyl-D-aspartate NR2B receptor antagonist in the 6-hydroxydopamine rat model of Parkinson's disease. Clinical and Experimental Pharmacology and Physiology, 35(11), 1388-1394.
  • Henderson, J., Lanciego, J., Smith, Y., Gundlach, A., Kassiou, M. (2008). Proceedings of the 2007 International Brain Research Organisation Satellite Meeting "Movement Disorders: Focus on the Thalamus and Basal Ganglia" held in Sydney, Australia, 10-11 July, 2007. Brain Research Bulletin, 78(2-3), 53-54.
  • Fulton, R., Kyme, A., Zhou, V., Leaver, K., Kassiou, M., Lehnert, W., Meikle, S. (2008). Progress towards microPET imaging of small, awake laboratory animals. 2008 World Molecular Imaging Congress, Europe: World Molecular Imaging Congress.
  • Guenther, K., Hambley, T., Kassiou, M. (2008). Radiolabelled probes for imaging multidrug resistance using single photon emission tomography (SPECT) and positron emission tomography (PET). In Nicola Antonio Colabufo (Eds.), Multidrug Resistance: Biological and Pharmaceutical Advances in Antitumour Treatment, (pp. 291-320). India: Research Signpost.
  • Damont, A., Hinnen, F., Kuhnast, B., Schollhorn-Peyronneau, M., James, M., Luus, C., Tavitian, B., Kassiou, M., Dolle, F. (2008). Radiosynthesis of [(18)F]DPA-714, a selective radioligand for imaging the translocator protein (18 kDa) PET. Journal of Labelled Compounds and Radiopharmaceuticals, 51(7-8), 286-292.
  • Dolle, F., Langle, S., Roger, G., Fulton, R., Lagnel, B., Henderson, D., Hinnen, F., Paine, T., Coster, M., Valette, H., Kassiou, M., et al (2008). Synthesis and In-Vivo Evaluation of [(11)C]p-PVP-MEMA as a PET Radioligand for Imaging Nicotinic Receptors. Australian Journal of Chemistry: an international journal for chemical science, 61(6), 438-445.

2007

  • Doorduin, J., Klein, H., James, M., Kassiou, M., Dierckx, R., Vries, E. (2007). (18F)DPA-714 as a novel PET tracer for PBR: A comparison with (11C)PK11195 in a rat model of HSV encephalitis. 17th International Symposium on Radiopharmaceutical Sciences. John Wiley & Sons.
  • Banister, S., Clegg, J., Coster, M., Jolliffe, K., Kassiou, M. (2007). (1R,2S,3R,6S,7R,8S)-Tricyclo[6.2.1.02,7]-undeca-4,9-diene-3,6-diol. Acta Crystallographica. Section E: Structure Reports Online, E63, o92-o93.
  • Emond, P., Mavel, S., Zea-Ponce, Y., Kassiou, M., Garreau, L., Bodard, S., Drossard, M., Chalon, S., Guilloteau, D. (2007). (E)-[125I]-5-AOIBV: a SPECT radioligand for the vesicular acetylcholine transporter. Nuclear Medicine and Biology, 34(8), 967-971.
  • Boutin, H., Chauveau, F., Thominiaux, C., Gregoire, M., James, M., Trebossen, R., Hantraye, P., Dolle, F., Tavitian, B., Kassiou, M. (2007). 11C-DPA-713: A novel peripheral benzodiazepine receptor PET ligand for in vivo imaging of neuroinflammation. The Journal of Nuclear Medicine, 48(4), 573-581.
  • Kozikowski, A., Chellappan, S., Henderson, D., Fulton, R., Giboureau, N., Xiao, Y., Wei, Z., Guilloteau, D., Emond, P., Dolle, F., Kassiou, M., et al (2007). Acetylenic pyridines for use in PET imaging of nicotinic receptors. ChemMedChem: chemistry enabling drug discovery, 2, 54-57.
  • Quinlivan, M., Chalon, S., Vergote, J., Henderson, J., Katsifis, A., Kassiou, M., Guilloteau, D. (2007). Decreased vesicular acetylcholine transporter and alpha-4beta-2 nicotinic receptor density in the rat brain following 192 IgG-saporin immunolesioning. Neuroscience Letters, 415, 97-101.
  • James, M., Fulton, R., Vercouille, J., Henderson, D., Garreau, L., Eberl, S., Chalon, S., Selleri, S., Dolle, F., Guilloteau, D., Kassiou, M. (2007). DPA-714 A new translocator protein (18kDa) ligand: Synthesis, radiofluorination and pharmacological characterisation. 17th International Symposium on Radiopharmaceutical Sciences. John Wiley & Sons.
  • Mavel, S., Zea-Ponce, Y., Garreau, L., Chalon, S., Kassiou, M., Guilloteau, D., Emond, P. (2007). E-((R,R) and (S,S))-5-(125I)-AOIBV: Potential SPECT tracers in vivo studies of the vesicular AcetylCholine Transporter (VACht). 17th International Symposium on Radiopharmaceutical Sciences. John Wiley & Sons.
  • Giboureau, N., Emond, P., Fulton, R., Henderson, D., Chalon, S., Garreau, L., Roselt, P., Eberl, S., Mavel, S., Bodard, S., Fulham, M., Kassiou, M., et al (2007). Ex vivo and in vivo evaluation of (2R,3R)-5-[18F]-fluoroethoxy- and fluoropropoxy-benzovesamicol, as PET radioligands for the vesicular acetylcholine transporter. Synapse (New York), 61(12), 962-670.
  • Naidoo (Naidoo-Variawa), S., Hey Cunningham, A., Lehnert, W., Kench, P., Kassiou, M., Banati, R., Meikle, S. (2007). High-resolution imaging of the large non-human primate brain using microPET: a feasibility study. Physics in Medicine and Biology, 52(22), 6627-6638.
  • Collier, T., Waterhouse, R., Kassiou, M. (2007). Imaging sigma receptors: Applications in drug development. Current Pharmaceutical Design, 13, 51-72.
  • Kassiou, M. (2007). Molecular imaging in drug development (Editorial). Current Pharmaceutical Design, 13(1), 1-1.
  • Gunosewoyo, H., Coster, M., Kassiou, M. (2007). Molecular probes for P2X7 receptor studies. Current Medicinal Chemistry, 14(14), 1505-1523.
  • Cagnin, A., Kassiou, M., Meikle, S., Banati, R. (2007). Positron emission tomography imaging of neuroinflammation. Neurotherapeutics, 4(3), 443-452.
  • Kassiou, M., Chellappan, S., Henderson, D., Fulton, R., Giboureau, N., Xiao, Y., Wei, Z., Guilloteau, D., Emond, P., Dolle, F., et al (2007). Radiosynthesis and preliminary evaluation of ZW-90 and ZW-110, two novel acetylenic pyridines for imaging nicotonic receptors. 17th International Symposium on Radiopharmaceutical Sciences. John Wiley & Sons.
  • Giboureau, N., Chalon, S., Garreau, L., Kassiou, M., Emond, P., Guilloteau, D. (2007). Rat distribution of (18F)-Fuoropropoxy- and (18F)-Fluoroethoxybenzovesamicol, as PET radioligands for the vesicular acetylcholine transporter (VACht). 17th International Symposium on Radiopharmaceutical Sciences. John Wiley & Sons.
  • Creelman, A., Thominiaux, C., Chauveau, F., Fulton, R., Kuhnast, B., Henderson, D., Boutin, H., Selleri, S., McGregor, I., Hantraye, P., Kassiou, M., et al (2007). Synthesis and evaluation of the translocator protein (18kDa) (TSPO) ligand (11C)DPA0715 in rat and non-human primate. 17th International Symposium on Radiopharmaceutical Sciences. John Wiley & Sons.
  • Langley, S., Roger, G., Fulton, R., Lagnel, B., Henderson, D., Hinnen, F., Bottlaender, M., Dolle, F., Kassiou, M. (2007). Synthesis and in vivo evaluation of (11c)P-PVP-MEMA as a PET radioligand for Imaging nicotonic receptors. 17th International Symposium on Radiopharmaceutical Sciences. John Wiley & Sons.
  • Liu, X., Banister, S., Christie, M., Banati, R., Meikle, S., Coster, M., Kassiou, M. (2007). Trishomocubanes: Novel sigma ligands modulate cocaine-induced behavioural effects. European Journal of Pharmacology, 555(1), 37-42.

2006

  • Truong, L., Allbutt, H., Kassiou, M., Henderson, J. (2006). Developing a preclinical model of Parkinson's disease: a study of behaviour in rats with graded 6-OHDA lesions. Behavioural Brain Research, 169(1), 1-9.
  • James, M., Selleri, S., Kassiou, M. (2006). Development of ligands for the peripheral benzodiazepine receptor. Current Medicinal Chemistry, 13(17), 1991-2001.
  • Thominiaux, C., Dolle, F., James, M., Bramoulle, Y., Boutin, H., Besret, L., Gregoire, M., Valette, H., Bottlaender, M., Tavitian, B., Kassiou, M., et al (2006). Improved synthesis of the peripheral benzodiazepine receptor ligand C-11 DPA-713 using C-11 methyl triflate. Applied Radiation and Isotopes, 64(5), 570-573.
  • Cagnin, A., Kassiou, M., Meikle, S., Banati, R. (2006). In vivo evidence for microglial activation in neurodegenerative dementia. Acta Neurologica Scandinavica, 114(Supplement 185), 107-114.
  • Thominiaux, C., de Bruin, B., Bramoulle, Y., Hinnen, F., Demphel, S., Valette, H., Bottlaender, M., Besret, L., Kassiou, M., Dolle, F. (2006). Radiosynthesis of (E)-N-(2- C-11 methoxybenzyl)-3-phenyl-acrylamidine, a novel subnanomolar NR2B subtype-selective NMDA receptor antagonist. Applied Radiation and Isotopes, 64(3), 348-354.
  • Assaad, T., Mavel, S., Parsons, S., Kruse, S., Galineau, L., Allouchi, H., Kassiou, M., Chalon, S., Guilloteau, D., Emond, P. (2006). Synthesis and in vitro evaluation of N-substituted aza-trozamicol analogs as vesicular acetylcholine transporter ligands. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 16(10), 2654-2657.
  • Vercouillie, J., Mavel, S., Galineau, L., Ragusa, T., Innis, R., Chalon, S., Kassiou, M., Dolle, F., Besnard, J., Guilloteau, D., et al (2006). Synthesis and in vitro evaluation of novel derivatives of diphenylsulfide as serotonin transporter ligands. Bioorganic and Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 16(5), 1297-1300.
  • Issa, F., Kassiou, M., Chan, H., McLeod, M. (2006). Synthesis and radiolabelling of ipratropium and tiotropium for use as PET ligands in the study of inhaled drug deposition. Australian Journal of Chemistry: an international journal for chemical science, 59(1), 53-58.
  • Liu, X., Banister, S., Christie, M., Banati, R., Meikle, S., Coster, M., Kassiou, M. (2006). Trishomocubanes: Novel Sigma ligands modulate cocaine-induced behavioural effects. European Journal of Pharmacology, 555(1), 37-42.

2005

  • Kassiou, M. (2005). Capabilities of PET and SPECT in pre-clinical and clinical research. Current Pharmaceutical Design, 11(25), 3201-3201.
  • Liu, X., Mattner, F., Katsifis, A., Christie, M., Kassiou, M. (2005). Influence of Trishomocubanes on Sigma Receptor Binding of N-(1-Benzylpiperidin- 4-yl)-4-[123I]iodobenzamide In Vivo in the Rat Brain. Medicinal Chemistry, 1(1), 31-38.
  • Kassiou, M., Meikle, S., Banati, R. (2005). Ligands for peripheral benzodiazepine binding sites in glial cells. Brain Research Reviews, 48(2), 207-210.
  • Kassiou, M., Bruin, B., Demphel, S., Besret, L., Hinnen, F., Dolle, F., Bramoulle, Y., Thominiaux, C., Bottlaender, M. (2005). Radiosynthesis of (E)-N-(2-[11C]methoxybenzyl)-3-phenyl-acrylamidine, a novel subnanomolar NR2B subtype-selective NMDA receptor ligand. 16th International Symposium on Radiopharmaceutical Chemistry, United Kingdom: Wiley.
  • Mohamed, A., Eberl, S., Fulham, M., Kassiou, M., Zaman, A., Henderson, D., Beveridge, S., Constable, C., Lo, S. (2005). Sequential 123I-iododexetimide scans in temporal lobe epilepsy: comparison with neuroimaging scans (MR imaging and F-18-FDG PET imaging). European Journal of Nuclear Medicine and Molecular Imaging, 32(2), 180-185.
  • Meikle, S., Kench, P., Kassiou, M., Banati, R. (2005). Small animal SPECT and its place in the matrix of molecular imaging technologies. Physics in Medicine and Biology, 50(22), R45-R61.
  • Zea-Ponce, Y., Mavel, S., Assaad, T., Kruse, S., Parsons, S., Emond, P., Chalon, S., Giboureau, N., Kassiou, M., Guilloteau, D. (2005). Synthesis and in vitro evaluation of new benzovesamicol analogues as potential imaging probes for the vesicular acetylcholine transporter. Bioorganic and Medicinal Chemistry: the tetrahedron journal for research at the interface of chemistry and biology, 13(3), 745-753.
  • Kassiou, M., Dannals, R., Liu, X., Wong, D., Ravert, H., Scheffel, U. (2005). Synthesis and in vivo evaluation of a new PET radioligand for studying sigma-2 receptors. Bioorganic and Medicinal Chemistry: the tetrahedron journal for research at the interface of chemistry and biology, 13(11), 3623-3626.
  • Fulham, M., Kassiou, M., Dolle, F., Thomson, S., Henderson, D., James, M., Eberl, S., Fulton, R., Allan, R. (2005). Synthesis and In Vivo Evaluation of a Novel Peripheral Benzodiazepine Receptor PET Radioligand. 16th International Symposium on Radiopharmaceutical Chemistry, United Kingdom: Wiley.
  • James, M., Fulton, R., Henderson, D., Eberl, S., Meikle, S., Thomson, S., Allan, R., Dolle, F., Fulham, M., Kassiou, M. (2005). Synthesis and in vivo evaluation of a novel peripheral benzodiazepine receptor PET radioligand. Bioorganic and Medicinal Chemistry: the tetrahedron journal for research at the interface of chemistry and biology, 13(22), 6188-6194.

2004

  • Henderson, D., Eberl, S., Thomson, S., Smith, A., Allan, R., Fulham, M., Loiacono, R., Kassiou, M. (2004). 3-Pyridyl Ethers As Spect Radioligands For Imaging Nicotinic Acetylcholine Receptors. Applied Radiation and Isotopes, 60(5), 669-676.
  • Katsifis, A., Kassiou, M. (2004). Development Of Radioligands For In Vivo Imaging Of Gaba(A)-Benzodiazepine Receptors. Mini - Reviews in Medicinal Chemistry, 4(8), 909-921.
  • Dolle, F., Valette, H., Demphel, S., Coulon, C., Ottaviani, M., Bottlaender, M., Kassiou, M. (2004). Radiosynthesis And In Vivo Evaluation Of [11C]Ro-547312: A Novel Nr1/2B Subtype Selective Nmda Receptor Radioligand. Journal of Labelled Compounds and Radiopharmaceuticals, 47(13), 911-920.
  • Roger, G., Dolle, F., de Bruin, B., Liu, X., Besret, L., Bramoulle, Y., Coulon, C., Ottaviani, M., Bottlaender, M., Valette, H., Kassiou, M. (2004). Radiosynthesis And Pharmacological Evaluation Of [11C]Emd-95885: A High Affinity Ligand For Nr2B-Containing Nmda Receptors. Bioorganic and Medicinal Chemistry: the tetrahedron journal for research at the interface of chemistry and biology, 12(12), 3229-3237.
  • Roselt, P., Meikle, S., Kassiou, M. (2004). The Role Of Positron Emission Tomography In The Discovery And Development Of New Drugs; As Studied In Laboratory Animals. European Journal of Drug Metabolism and Pharmacokinetics, 29(1), 1-6.

2003

  • Kassiou, M., Katsifis, A. (2003). PET radiochemistry in drug development and evaluation. Chemistry in Australia, 70(5), 10-12.
  • Katsifis, A., Mardon, K., Mattner, F., Loc'h, C., McPhee, M., Dikic, B., Kassiou, M., Ridley, D. (2003). Pharmacological evaluation of (S)-8-[123I]iodobretazenil: a radioligand for in vivo studies of central benzodiazepine receptors. Nuclear Medicine and Biology, 30(2), 191-198.
  • Feng, D., Kassiou, M., Fulham, M., Wong, K., Elberl, S. (2003). Quantification of 5-[123I]iodo-A-85380 in nonhuman primates using spect: parameter identifiability and stabilitty. Modelling and Control in Biomedical Systems 2003 (Including Biological Systems), UK: Pergamon.
  • Quinlivan, M., Mattner, F., Papazian, V., Zhou, J., Katsifis, A., Emond, P., Chalon, S., Kozikowski, A., Guilloteau, D., Kassiou, M. (2003). Synthesis and evaluation of iodine-123 labelled tricyclic tropanes as radioligands for the serotonin transporter. Nuclear Medicine and Biology, 30(7), 741-746.
  • Roger, G., Lagnel, B., Besret, L., Bramoulle, Y., Coulon, C., Ottaviani, M., Kassiou, M., Bottlaender, M., Valette, H., Dolle, F. (2003). Synthesis, radiosynthesis and In Vivo evaluation of 5-[3-(4-Benzylpiperidin-1-yl) prop-1-ynyl]-1, 3-dihydrobenzoimidazol-2-[11C] one, as a potent NR 1A/2B subtype selective NMDA PET radiotracer. Bioorganic and Medicinal Chemistry: the tetrahedron journal for research at the interface of chemistry and biology, 11, 5401-5408.

2002

  • Kassiou, M., Loc'h, C., Bottlaender, M., Mardon, K., Ottaviani, M., Coulon, C., Katsifis, A., Maziere, B. (2002). (+)-[76Br]A-69024: a non-benzazepine radioligand for studies of dopamine D1 receptors using PET. Nuclear Medicine and Biology, 29(3), 295-302.
  • Kassiou, M., Bottlaender, M., Loc'h, C., Dolle, F., Musachio, J., Coulon, C., Ottaviani, M., Dannals, R., Maziere, B. (2002). Pharmacological evaluation of a Br-76 analog of epibatidine: a potent ligand for studying brain nicotinic acetylcholine receptors. Synapse (New York), 45(2), 95-104.
  • Kassiou, M., Loc'h, C., Dolle, F., Musachio, J., Dolci, L., Crouzel, C., Dannals, R., Maziere, B. (2002). Preparation of a bromine-76 labelled analogue of epibatidine: a potent ligand for nicotinic acetylcholine receptor studies. Applied Radiation and Isotopes, 57(5), 713-717.

2001

  • Kassiou, M., Eberl, S., Meikle, S., Birrell, A., Constable, C., Fulham, M., Wong, D., Musachio, J. (2001). In vivo imaging of nicotinic receptor upregulation following chronic (-)-nicotine treatment in baboon using SPECT. Nuclear Medicine and Biology, 28, 165-175.
  • Kassiou, M., Mardon, K., Mattner,, F., Katsifis, A., Dikic, B. (2001). Pharmacological evaluation of (+)-2-[123I]A-69024: A radioligand for in vivo studies of dopamine D1 receptors. Life Sciences, 69, 669-675.
  • Liu, X., Christie, M., Kassiou, M., Nuwayhid, S., Werling, L. (2001). Trishomocubanes: Novel sigma-ligands modulate amphetamine-stimulated [3H]dopamine release. European Journal of Pharmacology, 422, 39-45.
  • Liu, X., Kassiou, M., Christie, M., Hambley, T. (2001). Trishomocubanes: requirements for sigma receptor binding and subtype selectivity. Australian Journal of Chemistry: an international journal for chemical science, 54, 31-36.
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Honours project opportunities

  • P2X7 RECEPTOR LIGANDS IN THE TREATMENT OF DEPRESSION
  • DEFINING THE INTERACTION OF THERAPEUTIC DRUGS AT THE TRANSLOCATOR PROTEIN
  • SIGMA LIGANDS AS NEUROPROTECTIVE AGENTS IN BRAIN DISEASE
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Keywords

Medicinal chemistry; Drug design; Pharmacology

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