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

Neuropsychopharmacology. 1996 Jan;14(1):19-25. doi: 10.1016/S0893-133X(96)80055-8.


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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Antidepressive Agents / metabolism
  • Depressive Disorder / metabolism
  • Humans
  • Receptors, Serotonin / metabolism*
  • Serotonin / metabolism
  • Signal Transduction*
  • Transcription, Genetic*


  • Antidepressive Agents
  • Receptors, Serotonin
  • Serotonin