Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors
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Roth, Bryan L, et al. Binding of Typical and Atypical Antipsychotic Agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 Receptors. 1994. https://doi.org/10.17615/74zp-ze10APA
Roth, B., Craigo, S., Choudhary, M., Uluer, A., Monsma, J., Shen, Y., Meltzer, H., & Sibley, D. (1994). Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. https://doi.org/10.17615/74zp-ze10Chicago
Roth, Bryan L., Sean C Craigo, M. Salman Choudhary, A Uluer, Jr Monsma, Y Shen, Herbert Y Meltzer et al. 1994. Binding of Typical and Atypical Antipsychotic Agents to 5-Hydroxytryptamine-6 and 5-Hydroxytryptamine-7 Receptors. https://doi.org/10.17615/74zp-ze10- Creator
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Roth, Bryan L.
- ORCID: https://orcid.org/0000-0002-0561-6526
- Other Affiliation: Laboratory of Biological Psychiatry, Department of Psychiatry, Case Western Reserve University School of Medicine, Cleveland, OH
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Craigo, Sean C.
- Other Affiliation: Laboratory of Biological Psychiatry, Department of Psychiatry, Case Western Reserve University School of Medicine, Cleveland, OH
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Choudhary, M. Salman
- Other Affiliation: Laboratory of Biological Psychiatry, Department of Psychiatry, Case Western Reserve University School of Medicine, Cleveland, OH
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Uluer, A.
- Other Affiliation: Laboratory of Biological Psychiatry, Department of Psychiatry, Case Western Reserve University School of Medicine, Cleveland, OH
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Monsma, Frederick J., Jr.
- Other Affiliation: Molecular Neuropharmacology Section, National Institutes of Neurological Disorders and Stroke, National Institutes of Health, Bethesda, MD
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Shen, Y.
- Other Affiliation: Molecular Neuropharmacology Section, National Institutes of Neurological Disorders and Stroke, National Institutes of Health, Bethesda, MD
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Meltzer, Herbert Y.
- Other Affiliation: Laboratory of Biological Psychiatry, Department of Psychiatry, Case Western Reserve University School of Medicine, Cleveland, OH
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Sibley, David R.
- Other Affiliation: Molecular Neuropharmacology Section, National Institutes of Neurological Disorders and Stroke, National Institutes of Health, Bethesda, MD
- Abstract
- The authors examined the affinities of 36 typical and atypical antipsychotic agents for the cloned rat 5-hydroxytryptamine-6 (5-HT6) and rat 5-hydroxytryptamine-7 (5-HT7) receptors in transiently expressed COS-7 cells (5-HT7) or stably transfected HEK-293 cells (5-HT6 receptors). Clozapine and several related atypical antipsychotic agents (rilapine, olanzepine, tiospirone, fluperlapine, clorotepine and zotepine) had high affinities for the newly discovered 5-HT6 receptor (Kis less than 20 nM). The 5-HT7 receptor bound clozapine, rilapine, fluperlapine, clorotepine, zotepine and risperidone but not tiospirone and olanzepine, with affinities less than 15 nM. In addition, several typical antipsychotic agents (chloroprothixene, chlorpromazine, clothiapine and fluphenazine) had high affinities for both the 5-HT6 and 5-HT7 receptors. Pimozide, a diphenylbutylpiperidine, had the highest affinity of all the typical antipsychotic agents tested for the 5-HT7 receptor (Ki = 0.5 nM). Three putative atypical antipsychotic agents melperone, amperozide and MDL 100907 did not bind with high affinities to either the 5-HT6 or 5-HT7 receptors (Kis > 50 nM). Several dopamine-selective antipsychotic agents (raclopride, rimcazole and penfluridol) had essentially no affinity for either the 5-HT6 or 5-HT7 receptors (Ki values > 5000 nM).
- Date of publication
- 1994
- DOI
- Identifier
- 2-s2.0-0028261434
- Related resource URL
- Resource type
- Article
- Rights statement
- In Copyright
- Journal title
- Journal of Pharmacology and Experimental Therapeutics
- Journal volume
- 268
- Journal issue
- 3
- Page start
- 1403
- Page end
- 1410
- Language
- English
- Version
- Postprint
- ISSN
- 0022-3565
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