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Brain Res Bull. 2001 Nov 15;56(5):441-51.

Paradoxical trafficking and regulation of 5-HT(2A) receptors by agonists and antagonists.

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  • 1Department of Biochemistry, Case Western Reserve University School of Medicine, Cleveland, OH 44106-4935, USA.

Abstract

5-Hydroxytryptamine(2A) (serotonin(2A), 5-HT(2A)) receptors are important for many physiologic processes including platelet aggregation, smooth muscle contraction, and the modulation of mood and perception. A large number of pharmaceutical agents mediate their actions, at least in part, by modulating the number and/or activity of 5-HT(2A) receptors. Drugs with action at 5-HT(2A) receptors are used in the treatment of many disorders, including schizophrenia, depression, and anxiety disorders. This review summarizes over two decades of research on the regulation of 5-HT(2A) receptors and provides a comprehensive review of numerous in vivo studies describing the paradoxical phenomenon of 5-HT(2A) receptor down-regulation by chronic treatment with antidepressants and antipsychotics. In addition, studies reporting antagonist-induced internalization of 5-HT(2A) receptors and other G protein-coupled receptors will be highlighted as a possible mechanism to explain this paradoxical down-regulation. Finally, a review of the cellular and molecular mechanisms that may be responsible for agonist-mediated desensitization and internalization of 5-HT(2A) receptors will be presented.

PMID:
11750789
[PubMed - indexed for MEDLINE]
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