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Neuropsychopharmacology. 1996 Jan;14(1):19-25.

The 5-HT1A receptor: signaling, desensitization, and gene transcription.

Author information

1
Department of Pharmacology and Therapeutics, McGill University, Montreal, Canada.

Abstract

The hypothesis that antianxiety or antidepressant agents (e.g., 5-HT1A agonists, 5-HT uptake blockers) exert their clinical actions via enhancement of serotonergic neurotransmission due to desensitization of 5-HT1A autoreceptors predicts that regulation of this receptor plays a crucial role in the therapeutic actions of these agents. A multidisciplinary strategy is described for the characterization of the 5-HT1A receptor at the level of cellular signaling mechanisms and genetic regulation, using heterologous expression of the cloned receptor in cell lines, site-directed mutagenesis, isolation of receptor-positive neuronal cell lines, and promoter analysis of the 5-HT1A receptor gene. These analyses will yield new insights into the possible mechanisms down-regulation of 5-HT1A receptor signaling, and may suggest novel sites of inherent defect involved in anxiety syndromes or major depression.

PMID:
8719026
DOI:
10.1016/S0893-133X(96)80055-8
[Indexed for MEDLINE]
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