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Binding of typical and atypical antipsychotic agents to transiently expressed 5-HT1C receptors.
Open accessAbstract
We determined the affinities of clozapine and 21 other typical and atypical antipsychotic agents for the cloned 5-hydroxytryptamine-1C (5-HT1C) receptor. For these studies, 5-HT1C receptors were transiently expressed in COS-7 cells using the vector pSVK3-5HT1C. We discovered that clozapine and several other putative typical and atypical antipsychotic agents (loxapine greater than tiosperone greater than SCH23390 greater than fluperlapine greater than rilapine greater than chlorpromazine) had relatively high affinities (7-30 nM) for the cloned 5-HT1C receptor. Other antipsychotic agents (risperidone greater than tenilapine greater than mesoridazine greater than thioridazine greater than cis-fluphenthixol) had intermediate affinities (30-100 nM), whereas many other antipsychotics (fluphenazine greater than spiperone greater than amperozide greater than melperone greater than thiothixene greater than haloperidol, metoclopramide, pimozide, domperidone, sulpiride) had low affinities (greater than 500 nM) for the cloned 5-HT1C receptor. The results indicate that although several putative atypical antipsychotic agents have high affinities for the cloned rat 5-HT1C receptor, the spectrum of drug binding does not correlate with the atypical nature of these compounds.
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Citations
Cited by
Roth, B. L. (2016) · Neuron · doi:10.1016/j.neuron.2016.01.040 · Cited by 1,742
Self-citationMapping of Brain Activity by Automated Volume Analysis of Immediate Early Genes
Renier, N., Adams, E. L., Kirst, C., Wu, Z., Azevedo, R., Kohl, J., Autry, A. E., Kadiri, L., Umadevi Venkataraju, K., Zhou, Y., et al. (2016) · Cell · doi:10.1016/j.cell.2016.05.007 · Cited by 918
The Effects of Clozapine, Risperidone, and Olanzapine on Cognitive Function in Schizophrenia
Meltzer, H. Y., & McGurk, S. R. (1999) · Schizophrenia Bulletin · doi:10.1093/oxfordjournals.schbul.a033376 · Cited by 1,020
Self-citationMolecular biology of 5-HT receptors
Boess, F. G., & Martin, I. L. (1994) · Neuropharmacology · doi:10.1016/0028-3908(94)90059-0 · Cited by 677
Mechanisms of action of atypical antipsychotic drugs: a critical analysis
Kinon, B. J., & Lieberman, J. A. (1996) · Psychopharmacology · doi:10.1007/bf02245602 · Cited by 317
Metadata
- Authors
- Roth, B. L., Ciaranello, R. D., & Meltzer, H. Y.
- Venue
- The Journal of Pharmacology and Experimental Therapeutics
- Publisher
- Elsevier BV
- Published
- 1992-03
- Volume
- 260
- Issue
- 3
- Pages
- 1361-1365
- ISSN
- 0022-3565 (ISSN-L)
- OpenAlex
- W1930849785
- Cited by
- 197
- References
- 0
- FWCI
- 15.70
- Type
- journal article
- Language
- en
- Open access
- green
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- Roth, B. L., Ciaranello, R. D., & Meltzer, H. Y. (1992). Binding of typical and atypical antipsychotic agents to transiently expressed 5-HT1C receptors. The Journal of Pharmacology and Experimental Therapeutics. https://doi.org/10.1016/s0022-3565(25)11452-3
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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