Receptor reserve for 5-hydroxytryptamine sub(1A)-mediated inhibition of serotonin synthesis: Possible relationship to anxiolytic properties of 5-hydroxytryptamine sub(1A) agonists

The irreversible receptor antagonist N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) was used to determine the relationship between receptor occupancy and response at central 5-hydroxytryptamine sub(1A) (5-HT sub(1A)) serotonin receptors mediating the inhibition of serotonin synthesis in rat c...

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Published inMolecular pharmacology Vol. 37; no. 2; pp. 231 - 237
Main Authors Meller, E, Goldstein, M, Bohmaker, K
Format Journal Article
LanguageEnglish
Published 01.01.1990
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Summary:The irreversible receptor antagonist N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) was used to determine the relationship between receptor occupancy and response at central 5-hydroxytryptamine sub(1A) (5-HT sub(1A)) serotonin receptors mediating the inhibition of serotonin synthesis in rat cortex and hippocampus. Because 5-HT sub(1A) receptor-mediated regulation of 5-HT synthesis appears to be mediated by somatodendritic autoreceptors on 5-HT neurons in the midbrain raphe nuclei, the results suggest that these autoreceptors possess a large receptor reserve for agonists. The relevance of these findings for the mechanism of action of nonbenzodiazepine anxiolytics is discussed.
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ISSN:0026-895X