Binding of typical and atypical antipsychotic agents to transiently expressed 5-HT(1C) receptors

B. L. Roth*, R. D. Ciaranello, H. Y. Meltzer

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

191 Scopus citations

Abstract

We determined the affinities of clozapine and 21 other typical and atypical antipsychotic agents for the cloned 5-hydroxytryptamine-1C (5- HT(1C))receptor. For these studies, 5-HT(1C) receptors were transiently expressed in COS-7 cells using the vector pSVK3-5HT(1C). We discovered that clozapine and several other putative typical and atypical antipsychotic agents (loxapine > tiosperone > SCH23390 > fluperlapine > rilapine > chlorpromazine) had relatively high affinities (7-30 nM) for the cloned 5- HT(1C) receptor. Other antipsychotic agents (risperidone > tenilapine > mesoridazine > thioridazine > cis-fluphenthixol) had intermediate affinities (30-100 nM), whereas many other antipsychotics (fluphenazine > spiperone > amperozide > melperone > thiothixene > haloperidol, metoclopramide, pimozide, domperidone, sulpuride) had low affinities (>500 nM) for the cloned 5-HT(1C) receptor. The results indicate that although several putative atypical antipsychotic agents have high affinities for the cloned rat 5-HT(1C) receptor, the spectrum of drug binding does not correlate with the atypical nature of these compounds.

Original languageEnglish (US)
Pages (from-to)1361-1365
Number of pages5
JournalJournal of Pharmacology and Experimental Therapeutics
Volume260
Issue number3
StatePublished - Jan 1 1992

ASJC Scopus subject areas

  • Pharmacology

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