Blockade of central 5-hydroxytryptamine receptors by methiothepin
| Autor: | Willy Haefely, M. A. Monachon, M. Jalfre, Willy P. Burkard |
|---|---|
| Rok vydání: | 1972 |
| Předmět: |
Bridged-Ring Compounds
Dibenzothiepins Serotonin 5-hydroxytryptamine receptors Receptors Drug Pharmacology Sulfides Inhibitory postsynaptic potential Piperazines Animals heterocyclic compounds Receptor Evoked Potentials CATS Chemistry Reticular Formation Antagonist Tryptophan Rats Inbred Strains General Medicine Hydroxyindoleacetic Acid Rat brain Blockade Rats Receptors Neurotransmitter Tranquilizing Agents Synapses Cats Female Serotonin Antagonists |
| Zdroj: | Naunyn-Schmiedeberg's archives of pharmacology. 274(2) |
| ISSN: | 0028-1298 |
| Popis: | Methiothepin (1-[10,11-dihydro-8-(methylthio)dibenzo[b,f] thiepin-10-yl]-4-methylpiperazine maleate), a representative of a new class of neuroleptics, is shown to be an antagonist of 5-hydroxytryptamine (5-HT) at receptors in the CNS. The neuropharmacological evidence was obtained by observing its effects on ponto-geniculo-occipital (PGO) spikes induced in curarized cats by either the benzoquinolizine Ro 4-1284 or p-chlorophenylalanine. Methiothepin a) increased the number of drug-induced spikes, b) antagonized the inhibitory action of 5-HTP and LSD on the spikas, and c) induced PGO-spikes by itself in untreated animals. The turnover of 5-HT in the rat brain was accelerated by methiothepin as indicated by virtually unaltered 5-HT levels, an increase of 5-hydroxyindole acetic acid, an enhancement of the 5-HT increase induced by a MAO inhibitor and by an increase of tryptophan levels in the brain. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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