Abstract
The hypothesis that antianxiety or antidepressant agents (e.g., 5-HT1A agonists, 5-HT uptake blockers) exert their clinical action 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 sties of inherent defect involved in anxiety syndromes or major depression.
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Albert, P., Lembo, P., Storring, J. et al. The 5-HT1A Receptor: Signaling, Desensitization, and Gene Transcription. Neuropsychopharmacol 14, 19–25 (1996). https://doi.org/10.1016/S0893-133X(96)80055-8
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DOI: https://doi.org/10.1016/S0893-133X(96)80055-8
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