Research Topics
| M KassiouSummaryAffiliation: University of Sydney Country: Australia Publications
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Detail Information
Publications
Synthesis and in vitro evaluation of new benzovesamicol analogues as potential imaging probes for the vesicular acetylcholine transporterYolanda Zea-Ponce
, INSERM U619, , 31 Av. Monge, 37200 Tours, France
Bioorg Med Chem 13:745-53. 2005..4 nM) and (E)-(S,S)-5-AOIBV (Kd=4.3 nM). (R,R)-3, and (R,R)-4 showed the same high affinity for VAChT as (-)-5-IBVM and may be suitable as imaging agents of cholinergic nerve terminals...- Preparation of a bromine-76 labelled analogue of epibatidine: a potent ligand for nicotinic acetylcholine receptor studiesM Kassiou
Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital, Camperdown, NSW, Australia
Appl Radiat Isot 57:713-7. 2002..The tracer purified by RP-HPLC was obtained in 70% radiochemical yield with a specific radioactivity of 20 GBq/micromol. Radiochemical and chemical purities measured by radio-TLC and HPLC were >98%... - Ligands for peripheral benzodiazepine binding sites in glial cellsMichael Kassiou
Ramaciotti Centre for Brain Imaging, Brain and Mind Research Institute BMRI, University of Sydney, NSW, Australia
Brain Res Brain Res Rev 48:207-10. 2005.... - Synthesis and in vivo evaluation of a new PET radioligand for studying sigma-2 receptorsMichael Kassiou
Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital, Missenden Rd, Camperdown, NSW 2050, Australia
Bioorg Med Chem 13:3623-6. 2005..The evaluation of this radioligand in vivo in the mouse clearly indicates that it does not possess the required properties for studying sigma-2 receptors in the brain using PET... - Pharmacological evaluation of a Br-76 analog of epibatidine: a potent ligand for studying brain nicotinic acetylcholine receptorsMichael Kassiou
Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital, Camperdown NSW 2050 Australia
Synapse 45:95-104. 2002..These preliminary results suggest that [(76)Br]BrPH has the potential to be a useful radioligand for studying the pharmacology of nicotinic acetylcholine receptors in preclinical experiments... - (+)-[76Br]A-69024: a non-benzazepine radioligand for studies of dopamine D1 receptors using PETMichael Kassiou
Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital, NSW 2050, Camperdown, Australia
Nucl Med Biol 29:295-302. 2002..These results suggest that (+)-[76Br]A-69024 may deserve further investigation as a potential radioligand for studying striatal and cortical dopamine D1 receptors using PET... - In vivo imaging of nicotinic receptor upregulation following chronic (-)-nicotine treatment in baboon using SPECTM Kassiou
Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital, Missenden Rd, Camperdown, NSW 2050, Australia
Nucl Med Biol 28:165-75. 2001..In this preliminary study, we have demonstrated for the first time in vivo upregulation of neuronal nAChR binding following chronic (-)-nicotine treatment... - Pharmacological evaluation of (+)-2- [123I]A-69024: a radioligand for in vivo studies of dopamine D1 receptorsM Kassiou
Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital, Camperdown, NSW, Australia
Life Sci 69:669-75. 2001..2-[123I]A-69024 displays enantioselectivity for dopamine D1 receptors and may deserve further investigation as a possible SPECT radioligand... - Attenuation correction for the large non-human primate brain imaging using microPETS Naidoo-Variawa
Discipline of Medical Radiation Sciences, Faculty of Health Sciences, University of Sydney, PO Box 170, Lidcombe, NSW 1825, Sydney, Australia
Phys Med Biol 55:2351-63. 2010.... - The influence of tomograph sensitivity on kinetic parameter estimation in positron emission tomography imaging studies of the rat brainS R Meikle
Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital, Sydney, Australia
Nucl Med Biol 27:617-25. 2000..We conclude that effective tomograph sensitivity of 3% may be an appropriate design goal for rat brain imaging... - Design, synthesis, and structure-affinity relationships of regioisomeric N-benzyl alkyl ether piperazine derivatives as sigma-1 receptor ligandsIman A Moussa
School of Chemistry, Discipline of Medical Radiation Sciences, University of Sydney, Sydney, NSW, Australia
J Med Chem 53:6228-39. 2010..The in vivo evaluation of [11C]13 indicates that this radiotracer is a suitable candidate for imaging the sigma1 receptor in neurodegenerative processes... - 3-Pyridyl ethers as SPECT radioligands for imaging nicotinic acetylcholine receptorsD J Henderson
Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital, Missenden Road, Camperdown, NSW, Sydney 2050, Australia
Appl Radiat Isot 60:669-76. 2004..3 nM, compared to the 5-bromo and 5-iodo compounds, 5 Ki =3.3 nM and 3 Ki =40.8 nM, respectively. Taken together, these results clearly indicate that 5-[123I]iodo-A-84543 is not suitable for the study of nAChRs in vivo using SPECT... - In vitro and in vivo characterisation of [3H]ANSTO-14 binding to the sigma 1 binding sitesV H Nguyen
Department of Pharmacology, The University of Sydney, NSW, Australia
Nucl Med Biol 26:209-15. 1999..Therefore, [3H]ANSTO-14 is a suitable ligand for labelling sigma 1 sites in vitro but is not suitable for brain imaging of sigma binding sites in vivo... - Evaluation of behavioural effects of a selective NMDA NR1A/2B receptor antagonist in the unilateral 6-OHDA lesion rat modelS T Warraich
Department of Pharmacology, Bosch Institute and School of Medical Sciences, University of Sydney, NSW 2006, Australia
Brain Res Bull 78:85-90. 2009..However levodopa-treated rats were slower than either controls or BZAD-01-treated rats in the locomotor test. The improvement in the apomorphine rotation test suggests that BZAD-01 may be a useful adjunct to levodopa monotherapy... - Developing a preclinical model of Parkinson's disease: a study of behaviour in rats with graded 6-OHDA lesionsL Truong
Department of Pharmacology, Institute for Biochemical Research, Bosch Building, School of Medical Sciences, University of Sydney, NSW 2006, Australia
Behav Brain Res 169:1-9. 2006..This graded model can be useful for testing potential neuroprotective compounds for PD... - Behavioural effects of a selective NMDA NR1A/2B receptor antagonist in rats with unilateral 6-OHDA+parafascicular lesionsL Truong
Department of Pharmacology, Bosch Building, Bosch Institute and School of Medical Sciences, University of Sydney, NSW 2006, Australia
Brain Res Bull 78:91-6. 2009..The latter was also improved by l-dopa in this model. These data support the use of selective NR1/NR2B NMDA antagonists in the therapeutics of PD... - Insights into structure-activity relationships and CNS therapeutic applications of NR2B selective antagonistsC Beinat
School of Chemistry, University of Sydney, NSW 2006, Australia
Curr Med Chem 17:4166-90. 2010..This review describes recent advances in the development of NR2B antagonists as well as their therapeutic applications... - Challenges in molecular imaging of Parkinson's disease: a brief overviewMichael Kassiou
Discipline of Medical Radiation Sciences, University of Sydney, NSW 2006, Australia
Brain Res Bull 78:105-8. 2009..This brief overview aims to outline the challenges and capabilities of PET and the more commonly used molecular probes in PD studies... - Decreased vesicular acetylcholine transporter and alpha(4)beta(2) nicotinic receptor density in the rat brain following 192 IgG-saporin immunolesioningMitchell Quinlivan
Universite Francois Rabelais de Tours, INSERM U619, Laboratoire de Biophysique Medicale et Pharmaceutique, 31 Avenue Monge, 37200 Tours, France
Neurosci Lett 415:97-101. 2007..The results with (125)I-A-85380 are unique and are in contrast with work performed in this animal model with other nAChR radioligands, indicating the favourable properties of this radioligand for molecular imaging... - Sequential 123I-iododexetimide scans in temporal lobe epilepsy: comparison with neuroimaging scans (MR imaging and 18F-FDG PET imaging)Armin Mohamed
Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital, Camperdown, NSW, 2050, Australia
Eur J Nucl Med Mol Imaging 32:180-5. 2005.... - High-resolution imaging of the large non-human primate brain using microPET: a feasibility studyS Naidoo Variawa
Discipline of Medical Radiation Sciences, Faculty of Health Sciences, University of Sydney, PO Box 170, Lidcombe, NSW 1825, Sydney, Australia
Phys Med Biol 52:6627-38. 2007..Further work to develop suitable correction algorithms for high-resolution large primate imaging is warranted... 
The nonpeptide oxytocin receptor agonist WAY 267,464: receptor-binding profile, prosocial effects and distribution of c-Fos expression in adolescent ratsC Hicks
School of Psychology, Brennan MacCallum Building, University of Sydney, Sydney, Australia
J Neuroendocrinol 24:1012-29. 2012..Antagonism of the V(1a) R by WAY 267,464 could underlie some of the prosocial effects of this drug either through a direct action or through disinhibition of oxytocin circuitry that is subject to vasopressin inhibitory influences...- Development of ligands for the peripheral benzodiazepine receptorMichelle L James
Department of Pharmacology, University of Sydney, NSW 2006, Australia
Curr Med Chem 13:1991-2001. 2006..This review highlights the main classes of PBR ligands to date. In addition the biological activity and therapeutic potential of certain PBR ligands is discussed... - Neuroprotective effects of a selective N-methyl-D-aspartate NR2B receptor antagonist in the 6-hydroxydopamine rat model of Parkinson's diseaseK R Leaver
Department of Pharmacology, Bosch Institute and School of Medical Sciences, University of Sydney, Sydney, New South Wales, Australia
Clin Exp Pharmacol Physiol 35:1388-94. 2008..Furthermore, there was no significant difference in any of the behavioural measures between lesioned rats pretreated with BZAD-01 and rats that underwent sham surgery... - DPA-714, a new translocator protein-specific ligand: synthesis, radiofluorination, and pharmacologic characterizationMichelle L James
Department of Pharmacology, University of Sydney, Sydney, New South Wales, Australia
J Nucl Med 49:814-22. 2008..Radioligands for the TSPO can therefore measure active disease in the brain. This article details the synthesis, radiofluorination, and pharmacologic evaluation of a new TSPO-specific pyrazolopyrimidine, DPA-714... - Behavioural effects of trishomocubanes in rats with unilateral 6-hydroxydopamine lesionsAddy van Dijk
Department of Pharmacology, Institute for Biomedical Research, School of Medical Sciences, Bosch Building, University of Sydney, NSW 2006, Australia
Behav Brain Res 190:14-21. 2008..vehicle treated rats so no neuroprotective effect was demonstrated in this model at the doses utilised... - Oxo-bridged isomers of aza-trishomocubane sigma (sigma) receptor ligands: Synthesis, in vitro binding, and molecular modelingSamuel D Banister
School of Chemistry, University of Sydney, NSW 2006, Australia
Bioorg Med Chem Lett 20:145-8. 2010..Molecular modeling was undertaken to rationalize these results... - Trishomocubanes: novel sigma ligands modulate cocaine-induced behavioural effectsXiang Liu
Department of Pharmacology, University of Sydney, NSW 2006, Australia
Eur J Pharmacol 555:37-42. 2007..The differential effect of TC1 and TC4 warrants further study of the mechanism of these actions. Present data also suggests a potential role for trishomocubane analogues in developing medication or research tools for cocaine addiction... - Purinergic P2X(7) receptor antagonists: Chemistry and fundamentals of biological screeningHendra Gunosewoyo
School of Chemistry, University of Sydney, NSW 2006, Australia
Bioorg Med Chem 17:4861-5. 2009..This perspective will attempt to highlight some of the most recent key findings in both the biology and chemistry... - Synthesis and evaluation of iodine-123 labelled tricyclic tropanes as radioligands for the serotonin transporterMitchell Quinlivan
Department of Pharmacology, University of Sydney, NSW 2006, Australia
Nucl Med Biol 30:741-6. 2003..In view of these results [(123)I]1 and [(123)I]2 do not appear to be suitable radioligands for in vivo studies of the SERT... - Synthesis and in vivo evaluation of a novel peripheral benzodiazepine receptor PET radioligandMichelle L James
Department of Pharmacology, University of Sydney, NSW 2006, Australia
Bioorg Med Chem 13:6188-94. 2005..Furthermore, [11C]1 represents the first ligand of its pharmacological class to be labelled for PET studies and therefore has the potential to generate new information on the pathological role of the PBR in vivo... - Cubyl amides: novel P2X7 receptor antagonistsHendra Gunosewoyo
School of Chemistry, University of Sydney, NSW 2006, Australia
Bioorg Med Chem Lett 18:3720-3. 2008..All synthesised compounds possessed P2X7R antagonistic properties when tested on rat spinal cord microglia cells. Extensive screening for binding to other neuroreceptor subtypes demonstrated their P2X7 selectivity... - P2X purinergic receptor ligands: recently patented compoundsHendra Gunosewoyo
University of Sydney, School of Chemistry, NSW 2006, Australia
Expert Opin Ther Pat 20:625-46. 2010..Their wide expression in the CNS, recent advances in the biochemical and pharmacological properties as well as increasing numbers of patents published in this research domain demand a review in this field... - Small animal SPECT and its place in the matrix of molecular imaging technologiesSteven R Meikle
School of Medical Radiation Sciences, Faculty of Health Sciences, University of Sydney, PO Box 170, Lidcombe, NSW 1825, Sydney, Australia
Phys Med Biol 50:R45-61. 2005.... - Radiosynthesis of (E)-N-(2-[11C]methoxybenzyl)-3-phenyl-acrylamidine, a novel subnanomolar NR2B subtype-selective NMDA receptor antagonistCyrille Thominiaux
, , CEA/DSV, , F-91401 Orsay, France
Appl Radiat Isot 64:348-54. 2006..8 to 1.2 Ci/micromol (29.6-44.4 GBq/micromol) at the end of radiosynthesis. No attempts were made to further optimise these reactions, as sufficient material was obtained to allow for preliminary pharmacological characterisation... - Acetylenic pyridines for use in PET imaging of nicotinic receptorsAlan P Kozikowski
Drug Discovery Program, Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, Illinois 60612, USA
ChemMedChem 2:54-7. 2007 - Development of radioligands for in vivo imaging of GABA(A)-benzodiazepine receptorsAndrew Katsifis
Radiopharmaceuticals Division R and D, Australian Nuclear Science and Technology Organisation, Private Mail Bag 1, Menai NSW 2234, Sydney, Australia
Mini Rev Med Chem 4:909-21. 2004.... - Synthesis, radiosynthesis and in vivo evaluation of 5-[3-(4-benzylpiperidin-1-yl)prop-1-ynyl]-1,3-dihydrobenzoimidazol-2-[(11)C]one, as a potent NR(1A)/2B subtype selective NMDA PET radiotracerGaelle Roger
Departement de Recherche Medicale, CEA DSV, 4 Place du General Leclerc, F 91401 Orsay, France
Bioorg Med Chem 11:5401-8. 2003..In view of these results, and especially considering the low brain penetration of the radiotracer, [(11)C]-1 does not have the required properties for imaging NMDA receptors using positron emission tomography... - Imaging sigma receptors: applications in drug developmentThomas Lee Collier
Siemens Biomarker Solutions, 406 Industrial Drive, North Wales, PA 19454, USA
Curr Pharm Des 13:51-72. 2007..This review provides an overview of the current knowledge of these sites with a focus on specific areas where in vivo sigma receptor imaging is currently being investigated... - Pharmacological evaluation of (S)-8-[123I]iodobretazenil: a radioligand for in vivo studies of central benzodiazepine receptorsAndrew Katsifis
Radiopharmaceuticals Division R and D, Australian Nuclear Science and Technology Organisation Menai NSW 2234, Sydney, Australia
Nucl Med Biol 30:191-8. 2003..S)-8-[(123)I]Iodobretazenil potently and selectively labels BZR in vivo and deserves further investigation as a possible SPECT radiotracer... - Dopamine D1 receptor imaging in the rodent and primate brain using the isoquinoline +-[11C]A-69024 and positron emission tomographyLaurent Besret
CNRS, URA 2210, 4 Place du General Leclerc, F 91406 Orsay, France
J Pharm Sci 97:2811-9. 2008..Thus, (+)-[(11)C]A-69024 appears to be a specific and enantioselective radioligand to visualize and quantify brain dopamine D1 receptors in vivo using positron emission tomography... - Ex vivo and in vivo evaluation of (2R,3R)-5-[(18)F]-fluoroethoxy- and fluoropropoxy-benzovesamicol, as PET radioligands for the vesicular acetylcholine transporterNicolas Giboureau
INSERM, U619, 37000 Tours, France
Synapse 61:962-70. 2007..The in vivo PET study of [(18)F]2 performed in baboon also revealed rapid defluorination as the main problem. Therefore [(18)F]1 and [(18)F]2 appear to be unsuitable for in vivo imaging of the VAChT using PET... - Influence of trishomocubanes on sigma receptor binding of N-(1-benzyl-piperidin-4-yl)-4-[123I]iodobenzamide in vivo in the rat brainXiang Liu
Department of Pharmacology The University of Sydney, NSW 2006 Australia
Med Chem 1:31-8. 2005..This demonstrates for the first time the ability of functionalised trishomocubanes to interact with sigma receptors in vivo... - (E)-[125I]-5-AOIBV: a SPECT radioligand for the vesicular acetylcholine transporterPatrick Emond
INSERM U619, 37000 Tours, France
Nucl Med Biol 34:967-71. 2007..These results made [125I]-( R,R)-5-AOIBV inferior to [125I]-IBVM for the VAChT exploration in vivo... - Synthesis and in vitro evaluation of N-substituted aza-trozamicol analogs as vesicular acetylcholine transporter ligandsThaer Assaad
, 37200 Tours, France
Bioorg Med Chem Lett 16:2654-7. 2006..These compounds will be soon radiolabeled with [(125)I] for further biological evaluation using single photon emission computed tomography (SPECT)... - Positron emission tomography imaging of neuroinflammationAnnachiara Cagnin
Department of Neuroscience, University of Padova, Via Giustiniani 5, 35128, Padova, Italy
Neurotherapeutics 4:443-52. 2007.... - The role of positron emission tomography in the discovery and development of new drugs; as studied in laboratory animalsPeter Roselt
Centre for Positron Emission Tomography, Peter MacCallum Cancer Centre East Melbourne, Australia
Eur J Drug Metab Pharmacokinet 29:1-6. 2004..Consequently PET imaging of rodents is emerging as a cost effective means of screening new pharmaceuticals and decreasing the time required for new drug development... - Molecular probes for P2X7 receptor studiesHendra Gunosewoyo
School of Chemistry, University of Sydney, NSW 2006 Australia
Curr Med Chem 14:1505-23. 2007..This article will review P2X7R ligands discovered to date, together with their biological activity and therapeutic potential... - 11C-DPA-713: a novel peripheral benzodiazepine receptor PET ligand for in vivo imaging of neuroinflammationHerve Boutin
CEA, Institut d Imagerie Biomédicale, Service Hospitalier Frederic Joliot, Laboratoire d Imagerie Moleculaire Experimentale, Orsay, France
J Nucl Med 48:573-81. 2007..Here we investigated a new PBR ligand suitable for PET to monitor neuroinflammatory processes as an indirect hallmark of neurodegeneration... - Synthesis and in vitro evaluation of novel derivatives of diphenylsulfide as serotonin transporter ligandsJohnny Vercouillie
, INSERM U619, , 31 Avenue Monge, 37200 Tours, France
Bioorg Med Chem Lett 16:1297-300. 2006..Three of these exhibited good to high in vitro affinity (0.5 nM < K(i) < 11 nM) and selectivity for the SERT over the other monoamine transporters...