PAST PROJECTS

2011

Martin, A; Boisgard, R; Kassiou, M; Dollé, F and Tavitian, B. (2011)
Reduced PBR/TSPO expression after minocycline treatment in a rat model of focal cerebral ischemia: A PET study using [18F]DPA-714.
Molecular Imaging and Biology, 13 (1), 10-15, 2011. DOI: 10.1007/s11307-010-0324-y

Banister, SD; Moussa, IA; Beinat, C; Reynolds, AJ; Schiavini, P; Jorgensen, WT and Kassiou, M. (2011)
Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands.
Bioorganic & Medicinal Chemistry Letters, 21 (1), 38-41, 2011. DOI: 10.1016/j.bmcl.2010.11.075

Issa, F, Kassiou, M, Rendina, L M (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, Vail, A, Prenant, C, Julyan, P, Maroy, R, Brown, G, Smigova, A, Herholz, K, Kassiou, M Crossman, D, Francis, S, Proctor, S, Russell, J, Hopkins, S, Tyrrell, P, Rothwell, N, Allan, S (2011)
Brain inflammation is induced by co-morbidities and risk factors for stroke,
Brain, Behavior, and Immunity, 25(6), 1113-1122

Moussa, I A, Banister, S D, Akladios, F.N., Chua, S W, Kassiou, M (2011)
Effects of linker elongation in a series of N-(2-benzofuranylmethyl)-N'-(methoxyphenylalkyl)piperazine sigma(1) receptor ligands,
Bioorganic & Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(19), 5707-5710

Banister, S D, Moussa, I A, Jorgensen, W.T., 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 () receptor ligands modulates off-target activity and subtype selectivity,
Bioorganic & Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(12), 3622-3626

Boucher, A A, Arnold, J C, Hunt, G E, Spiro, A, Spencer, J R, Brown, C, McGregor, I S, Bennett, M R, Kassiou, M (2011)
Resilience and Reduced C-FOS Expression in P2X7 Receptor Knockout Mice Exposed to Repeated Forced Swim Test,
Neuroscience, 189, 170-177

Damont, A, Boisgard, R, Kuhnast, B, Lemee, F, Raggiri, G, Scarf, A M, Da Pozzo, E, Selleri, S, Martini, C, Tavitian, B, Kassiou, M, Dolle, F (2011)
Synthesis of 6-[(18)F]fluoro-PBR28, a novel radiotracer for imaging the TSPO 18 kDa with PET,
Bioorganic & Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(16), 4819-4822

Scarf, A M, Kassiou, M (2011)
The translocator protein
The Journal of Nuclear Medicine, 52(5), 677-680

Banister, S D, Yoo, D.T., Chua, S W, Cui, J, Mach, R, Kassiou, M (2011)
N-arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (sigma) receptor ligands
Bioorganic & Medicinal Chemistry Letters: the tetrahedron journal for research at the interface of chemistry and biology, 21(18), 5289-5292


2010

Beinat, C; Banister, S; Moussa, I; Reynolds, AJ; McErlean, CSP and Kassiou, M.
Insights into structure-activity relationships and CNS therapeutic applications of NR2B selective antagonists.
Current Medicinal Chemistry, 17 (34), 4166-4190, 2010. DOI: 10.2174/092986710793348572

Morrison DE, Issa F, Bhadbhade M, Groebler L, Witting PK, Kassiou M, Rutledge PJ, Rendina LM. (2010)
Boronated phosphonium salts containing arylboronic acid, closo-carborane, or nido-carborane: synthesis, X-ray diffraction, in vitro cytotoxicity, and cellular uptake.
J. Biol. Inorg. Chem (in print)

Giboureau N, Som IM, Boucher-Arnold A, Guilloteau D Kassiou M. (2010)
PET Radioligands for the Vesicular Acetylcholine Transporter (VAChT).
Curr Top Med. Chem. 10 (15): 1569-83.

Reynolds A, Hanani R, Hibbs D, Damont A, Da Pozzo E, Selleri S, Dolle F, Martini C and Kassiou M. (2010)
Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO). Bioorg. Med. Chem Lett. 20 (19): 5799-5802.

Moussa IA, Banister SD, Beinat C, Giboureau N, Reynolds AJ and Kassiou M (2010)
Design, synthesis, and structure-affinity relationships of regioisomeric N-benzyl aklyl ether poperazine derivatives as s-1 receptor ligands.
J. Med. Chem. 53 (16): 6228-6239.

Luus C, Hanani R, Reynolds A and Kassiou M. (2010)
The development of PET radioligands for imaging the translocator protein (18 kDa): What have we learned?
J. Labelled Compounds & Radiopharm. 53 (7): 501-510.

Gunosewoyo H and Kassiou M (2010)
P2X purinergic receptor ligands: Recently patented compounds.
Expert Opin Ther Pat. 20 (5): 625-646.

Naidoo-Variawa S, Lehnert W, Kassiou M, Banati R and Meikle SR. (2010)
Attenuation correction for the large non-human primate brain imaging using microPET.
Phys. Med. Biol. 55 (8): 2351-2363.

Martin A, Boisgard R, Theze B, van Camp N, Kuhnast B, Damont A, Kassiou M, Dolle F and Tavitian B.
Evaluation of the PBR/TSPO radioligand [18F]DPA-714 in a rat model of focal cerebral ischemia.
J. Cereb. Blood Flow Metab. 30 (1): 230-241.

Banister SD, Moussa IA, Jordan MJT, Coster MJ and Kassiou M. (2010)
Oxo-bridged isomers of aza-trishomocubane sigma (sigma) receptor ligands: Synthesis, in vitro binding and molecular modeling.
Bioorg. Med. Chem Lett. 20 (1): 145-148.

Giboureau, N, Aumann, K M, 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 D, Roeda, D, Dolle, F, Kassiou, M (2010)
Fluorine-18 chemistry for PET: A concise introduction,
Current Radiopharmaceuticals, 3(2), 68-80

Carson, D S, Hunt, G E, Guastella, A, Barber, L, Cornish, J, Arnold, J C, Boucher, A A, McGregor, I S (2010)
Systemically administered oxytocin decreases methamphetamine activation of the subthalamic nucleus and accumbens core and stimulates oxytocinergic neurons in the hypothalamus
Addiction Biology, 15(4), 448-463


2009

ngton AR, McKinzie AA, Reynolds AJ, Kassiou M, Ryan RM and Vandenberg RJ. (2009)
Extracellular loops 2 and 4 of GLYT2 and required for N-arachidonylglycine inhibition of glycine transport.
J. Bio. Chem. 284 (52): 36424-36430.

Leaver KR, Allbutt HN, Creber NJ, Kassiou M and Henderson JM. (2009)
Oral pre-treatment with epigallocetechni gallate in 6-OHDA lesioned rats produces subtle symptomatic relief but not neuroprotection.
Brain. Res. Bull. 80 (6): 397-402.

Reynolds AJ and Kassiou M. (2009)
Recent advances in the Mitsunobu reaction: Modifications and applications to biologically active molecules.
Curr. Organic Chem. 13 (16): 1610-1632.

Ioppolo JA, Kassiou M and Redina LM. (2009)
Water-soluble phosphonium salts containing 1,12-dicarba-closo-dodecaborane (12).
Tetrahedron Letters 50(47): 6457-6461.

Valette H, Xiao Y, Peyronneau M-A, Damont A, Kozikowski AP, Wei Z-L, Kassiou M, Kellar KJ, Dolle F and Bottlaender M. (2009)
18F-ZW-104: A new radioligand for imaging neuronal nicotinic acetylcholine receptors - in vitro binding properties and PET studies in baboons.
J. Nucl. Med. 50 (8): 1349-1355.

Endres CJ, Pomper MG, James M, Uzuner O, Hammoud DA, Watkins CC, Reynolds A, Hilton J, Dannals RF and Kassiou M (2009)
Initial evaluation of 11C-DPA-713, a novel TSPO PET ligand, in humans.
J. Nucl. Med. 50 (8): 1276-1282.

Dolle F, Luus C, Reynolds A and Kassiou M (2009)
Radiolabelled molecules for imaging the translocator protein (18 kDa) using positron emission tomography
Curr. Med. Chem. 16 (22), 2899-2923.

Gunosewoyo H, Coster MJ, Bennett MR and Kassiou M (2009)
Purinergic P2X(7) receptor antagonists: Chemistry and fundamentals of biological screening
Bioorg. Med. Chem. 17 (14), 4861-4865.

Kassiou M, Banati R, Holsinger DRM, Meikle S (2009)
Challenges in molecular imaging of Parkinson’s disease: A brief overview
Brain Res. Bull. 78, 105-108.

Warraich ST, Allbutt HN, Billing R, Radford J, Coster MJ, Kassiou M and Henderson JM (2009)
Evaluation of behavioural effects of a selective NMDA NR1A/2B receptor antagonist in the unilateral 6-OHDA lesion rat model
Brain Res. Bull. 78, 85-90.

Truong L, Allbutt HN, Coster MJ, Kassiou M, Henderson JM (2009)
Behavioural effects of a selective NMDA NR1A/2B receptor antagonist in rats with unilateral 6-OHDA + parafascicular lesions
Brain Res. Bull. 78, 91-96.

Scarf AM, Ittner LM, Kassiou M (2009)
The translocator protein (18 kDa): Central nervous system disease and drug design
J. Med. Chem. 52, 581-592.

Chauveau F, Van Camp N, Dollé F, Kuhnast B, Thominiaux C, Hinnen F, e Damont A, Boutin H, James M, Kassiou M, Tavitian B (2009)
Comparative evaluation of the TSPO (18kDa)/PBR radioligands [11C]DPA-713, [18F]DPA-714, and [11C]PK11195 in a rat model of acute neuroinflammation
J. Nucl. Med. Mar;50(3):468-76

Doorduin J, Klein HC, Dierckx RA, James M, Kassiou M, de Vries EFJ. (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
Mol Imaging Biol 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

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

Besret L, Dollé F, Hérard A-S, Guillermier M, Coulon C, Ottaviani M, Bottlaender M, Hantraye P, Kassiou M (2008)
Dopamine D1 receptors imaging in the rodent and primate brain using (+)-[11C]A-69024 and positron emission tomography
J Pharm Sci 97, 2811-2819.

Van Dijk A, Johnston C, Allbutt HN, Kassiou M, Henderson JM. (2008)
Behavioural effects of trishomocubanes in rats with unilateral 6-hydroxydopamine lesions
Behav. Brain Res. 190, 14-21.

James ML, Fulton RR, Vercoullie J, Henderson DJ, Garreau L, Chalon S, Dolle F, Selleri S, Guilloteau D, Kassiou M (2008)
DPA-714, a new translocator protein (18kDa) (TSPO) ligand: Synthesis, radio-fluorination and pharmacological characterization
J. Nucl. Med. 49, 814-822.

Dollé F, Langle S, Roger G, Fulton RR, Lagnel-de Bruin B, Henderson DJ, Hinnen F, Paine T, Coster MJ, Valette H, Bottlaender M, Kassiou M (2008)
Synthesis and In Vivo Evaluation of [11C]p-PVP-MEMA as a PET Radioligand for Imaging Nicotinic Receptors
Aust. J. Chem. 61, 438-445.

Damont A, Hinnen H, Kuhnast B, Schollhorn-Peyronneau M, James M, Christopher Luus C,Tavitian B, Kassiou M, Dolle F (2008)
Radiosynthesis of [18F]DPA-714, a selective radioligand for imaging the translocator protein (18 kDa) with PET
J. Label. Compds. Radiopharm. 51, 286-292.

Gunosewoyo H, Guo JL, Bennett MR, Coster MJ, Kassiou M (2008)
Cubyl Amides: Novel P2X7 Receptor Antagonists
Bioorg. Med.Chem. Lett. 18, 3720-3723.

Leaver KR, Allbutt HN, Creber NJ, Kassiou M, Henderson JM (2008)
Neuroprotective effects of a selective NMDA NR2B receptor antagonist in the 6-OHDA rat model of Parkinson’s disease
Clin. Exp. Pharmacol. Physiol. 35, 1388-1394.

Guenther K, Hambley TW and Kassiuo M. Radiolabelled probes for imaging multidrug resistance using single photon emission tomography (SPECT) and positron emission tomography (PET). Book chapter in: Multidrug Resistance: Biological and Pharmaceutical Advances in Antitumour Treatment. ISBN: 978-81-308-0258-9, Editor: Nicola Antonio Colabufor, Publisher: Research Signpost, Volume 1, 291-320, 2008.


2007

Banister SD, Clegg JK, Coster MJ, Jolliffe KA, Kassiou M (2007)
(1R,2S,3R,6S,7R,8S)-Tricyclo[6.2.1.02,7]-undeca-4,9-diene-3,6-diol
Acta Cryst. 63, 92-93.

Liu X, Banister SD, Christie MJ, Banati R, Meikle S, Coster MJ, Kassiou M (2007)
Trishomocubanes: Novel Sigma ligands modulate cocaine-induced behavioural effects
Eur J Pharmacol 555, 37-42.

Kozikowski AP, Chellappan SK, Henderson D, Fulton R, Giboureau N, Xiao, Y, Wei ZL, Guilloteau D, Emond P, Dolle F, Kellar KJ, Kassiou M (2007)
Novel acetylenic pyridines for use in PET imaging of nicotinic receptors
ChemMedChem. 2, 54-57.

Quinlivan M, Chalon S, Vergote J, Henderson J, Katsifis A, Kassiou M, Guilloteau D. (2007)
Decreased vesicular acetylcholine transporter and alpha(4)beta(2) nicotinic receptor density in the rat brain following 192 IgG-saporin immunolesioning
Neurosci Lett 415, 97-101.

Boutin H, Chauveau F, Thominiaux C, Kuhnast B, Gregoire MC, James M, Jan S, Brulon V, Fontyn Y, Selleri S, 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
J. Nucl. Med. 48, 573–581.

Emond P, Mavel S, Zea-Ponce Y, Kassiou M, Garreau L, Bodard S, Marie-Laure Drossard ML, Chalon S, Guilloteau D (2007)
(E)-[125I]-5-AOIBV: a SPECT radioligand for the vesicular acetylcholine transporter
Nucl. Med. Biol. 34 967-971.

Giboureau N, Emond P, Fulton R, Henderson D, Chalon S, Garreau L, Roselt P, Eberl S, Mavel S, Bodard S, Fulham M, Guilloteau D, Kassiou M (2007)
Ex vivo & in vivo evaluation of (2R, 3R)-5-[18F]-fluoroethoxy- & fluoropropoxy-benzovesamicol, as PET radioligands for the vesicular acetylcholine transporter
Synapse 61 962-969.

Naidoo-Variawa S, Hey-Cunningham AJ, Lehnert W, Kench PL, Kassiou M, Banati R, Meikle SR (2007)
High resolution imaging of the large non-human primate brain using microPET: A feasibility study
Phys. Med. Biol. 52 6627-6638.

Waterhouse RN, Collier TL, Kassiou M (2007)
Imaging sigma receptors: Applications in drug development
Curr. Pharm. Design 13, 51-72.


2006

James M, Selleri S, Kassiou M (2006)
Ligands for Peripheral Benzodiazepine Receptors
Curr. Med. Chem. 13, 1991-2001.

Thominiaux C, Bruin B, Bramoulle Y, Hinnen F, Demphel S, Bottlaender M, Besret L, Kassiou M, Dolle F (2006)
Radiosynthesis of (E)-N-(2-[11C]methoxybenzyl)-3-phenyl-acrylamidine, a novel subnanomolar NR2B subtype-selective NMDA receptor ligand
Appl. Rad. Isotop. 64, 348-354.

Vercouillie J, Mavel S, Galineau L, Ragusa T, Innis R, Kassiou M, Chalon S, Dollé F, Besnard J-C, Guilloteau D, Emond P (2006)
Synthesis and in vitro evaluation of novel diphenylsulfide derivatives as serotonin transporter ligands
Bioorg. Med.Chem. Lett. 16, 1297-1300.

Truong L, Allbutt H, Kassiou M, Henderson JM (2006)
Developing a preclinical model of Parkinson’s disease: A study of behaviour in rats with graded 6-OHDA lesions
Behav. Brain Res. 169, 1-9.

Issa F, Kassiou M, Chan H-K, McLeod MD (2006)
Synthesis and Radiolabelling of Ipratropium and Tiotropium as PET Ligands for the Study of Inhaled Drug Deposition
Aust. J. Chem. 56, 53-58.

Thominiaux C, Dollé F, James ML, Bramoullé Y, Boutin H, Besret L, Grégoire MC, Valette H, Bottlaender M, Tavitian B, Hantraye P, Kassiou M (2006)
Improved Synthesis of the Peripheral Benzodiazepine Receptor Ligand (11C)DPA-713 using (11C)Methyl triflate
Appl. Rad. Isotop. 64, 570-573.

Assard T, Mavel S, Parsons SM, 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
Bioorg. Med.Chem. Lett. 16, 2654-2657.

Cagnin A, Kassiou M, Meikle SR, Banati RB (2006)
Clinical evidences of microglial activation in neurodegenerative dementia
Acta. Neurologic Scand 114,107-114.


2005

Mohamed A, Eberl S, Fulham MJ, Kassiou M, Zaman A, Henderson D, Beveridge S, Constable C, Lo SK (2005)
Sequential 123I-Iododexitimide (IDEX) Scans in Temporal Lobe Epilepsy: A comparison to Neuroimaging Scans (MR and 18F-fluorodeoxyglucose (FDG) PET imaging)
Eur. J. Nuc. Med. 32, 180-185.

Zea-Ponce Y, Mavel S, Assaad T, Emond P, Chalon S, Kruse S, Parsons SM, 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
Bioorg. Med. Chem. 13, 745-753.

Liu X, Mattner F, Katsifis A, Christie MJ, [Kassiou M (2005)
Influence of trishomocubanes on sigma receptor binding of N-(1-benzyl-piperidin-4-yl)-4-[123I]iodobenzamide in vivo in the rat brain
Med. Chem. 1, 31-38.

Kassiou M, Dannals RF, Liu X, Wong DF, Ravert RT, Scheffel UA (2005
Synthesis and in vivo evaluation of a new PET radioligand for studying sigma-2 receptors
Bioorg. Med. Chem. 13, 3623-3626.

James ML, Fulton RR, Henderson DJ, Eberl S, Meikle SR, Thomson S, Allan RD, Dolle F, Fulham MJ, Kassiou M (2005)
Synthesis and In Vivo Evaluation of a Novel Peripheral Benzodiazepine Receptor PET Radioligand
Bioorg. Med. Chem. 6188-6194.

Kassiou M, Meikle SR, Banati RB (2005)
Ligands for the peripheral benzodiazepine binding sites in glial cells
Brain Res. Rev. 48, 207-210.

Meikle SR, Kench P, Kassiou M, Banati RB (2005)
Small animal SPECT and its place in the matrix of molecular imaging technologies
Phys. Med. Biol. 50, R45-R61.