PMID: 7542051Mar 1, 1995Paper

Effect of clozapine and risperidone on 5-HT2 and D2-dopamine receptor binding in the post-mortem human brain. An autoradiographic study

European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology
H HallG Sedvall

Abstract

Effects of the antipsychotics risperidone and clozapine on 5-HT2 and D2-dopamine receptor binding were examined using [3H]N-methylspiperone ([3H]NMSP) and in vitro receptor autoradiography on human whole hemisphere cryosections. The 5-HT2 receptor antagonist ketanserin and the D2-dopamine receptor antagonist raclopride were used as references. [3H]NMSP binding was observed in caudate nucleus, putamen, and cerebral cortex indicating binding to D2-dopamine and 5-HT2 receptors. Risperidone and clozapine counteracted the binding to both receptor types. This was in contrast to raclopride, which selectively blocked the D2-dopamine receptors in the basal ganglia, and ketanserin, which selectively blocked the 5-HT2 receptors in the cerebral cortex. Risperidone (100 nM and 10 microM) blocked up to 90% of [3H]NMSP binding to both receptor types, whereas the blocking capacity of clozapine (10 microM) was lower (approximately 60%). The lack of total blockade of D2-dopamine receptors is in line with results obtained in with [11C]raclopride and positron emission tomography studies of clozapine treated human subjects. However, autoradiographic studies of clozapine competition of [3H]raclopride binding show total displacement of the binding at...Continue Reading

References

Jan 1, 1991·Journal of Neuroscience Methods·A PerssonG Sedvall
Dec 1, 1994·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·H HallL Farde
Jan 1, 1993·Psychopharmacology·A L NordströmC Halldin

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Citations

Mar 1, 1996·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·M M MarcusT H Svensson
Jan 31, 2004·Progress in Neuro-psychopharmacology & Biological Psychiatry·Yung-Chieh YenMian-Yoon Chong
Jan 31, 2004·Progress in Neuro-psychopharmacology & Biological Psychiatry·Philip HeiserHelmut Vedder
Jun 6, 2000·Pharmacology, Biochemistry, and Behavior·M Rodríguez-AriasJ Miñarro
Dec 1, 1996·Epilepsy Research·J R StevensP Szot
Oct 17, 2013·Progress in Neuro-psychopharmacology & Biological Psychiatry·Mary V Seeman, Philip Seeman
Sep 29, 2000·Artificial Cells, Blood Substitutes, and Immobilization Biotechnology·H AbeK Ikebuchi
Aug 17, 2021·Journal of Clinical Pharmacology·James R Docherty, Hadeel A Alsufyani

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