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 language | English (US) |
|---|---|
| Pages (from-to) | 1361-1365 |
| Number of pages | 5 |
| Journal | Journal of Pharmacology and Experimental Therapeutics |
| Volume | 260 |
| Issue number | 3 |
| State | Published - 1992 |
ASJC Scopus subject areas
- Molecular Medicine
- Pharmacology