Interaction of the atypical neuroleptic clozapine with 5-HT3 receptors in the cerebral cortex and superior cervical ganglion of the rat
| Autor: | K. J. Watling, Josephine A. Stanton, Margaret S. Beer, Nigel R. Newberry |
|---|---|
| Rok vydání: | 1990 |
| Předmět: |
Male
Fluphenazine Superior cervical ganglion medicine.medical_specialty Spiperone Indoles medicine.drug_class medicine.medical_treatment Tropisetron Atypical antipsychotic In Vitro Techniques Internal medicine medicine Haloperidol Animals Antipsychotic Clozapine 5-HT receptor Cerebral Cortex Pharmacology Ganglia Sympathetic Chemistry Rats Inbred Strains Rats Kinetics Endocrinology Receptors Serotonin Antipsychotic Agents Tropanes medicine.drug |
| Zdroj: | European Journal of Pharmacology. 182:465-472 |
| ISSN: | 0014-2999 |
| Popis: | Clozapine, an atypical neuroleptic drug devoid of extrapyramidal side effects, was a moderately potent, competitive inhibitor of the binding of [ 3 H]quaternised ICS 205–930 to 5-HT 3 receptor sites in rat cortical membranes, possessing a pK i value of 7.0. In contrast, several other antipsychotic agents, including fluphenazine, α-flupenthixol, haloperidol, spiperone and (-)-sulpiride were essentially inactive. Clozapine also antagonised the 2-methyl 5-HT-induced depolarisation of the rat isolated superior cervical ganglion, a response known to be mediated via 5-HT 3 receptors. Clozapine (0.1–1 μM) induced parallel displacements to the right of the dose-response curve to 2-methyl 5-HT in this tissue, possessing a pK b value of 7.3. These data suggest that the atypical antipsychotic profile of clozapine may be related, at least, in part to its ability to interact with central 5-HT 3 receptor sites. |
| Databáze: | OpenAIRE |
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