Abstract
5-Hydroxytryptamine2A (serotonin2A, 5-HT2A) 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-HT2A receptors. Drugs with action at 5-HT2A 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-HT2A receptors and provides a comprehensive review of numerous in vivo studies describing the paradoxical phenomenon of 5-HT2A receptor down-regulation by chronic treatment with antidepressants and antipsychotics. In addition, studies reporting antagonist-induced internalization of 5-HT2A 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-HT2A receptors will be presented.
Original language | English (US) |
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Pages (from-to) | 441-451 |
Number of pages | 11 |
Journal | Brain Research Bulletin |
Volume | 56 |
Issue number | 5 |
DOIs | |
State | Published - Nov 15 2001 |
Externally published | Yes |
Keywords
- Antidepressant
- Antipsychotic
- Arrestin
- Clozapine
- Down-regulation
- Internalization
ASJC Scopus subject areas
- Neuroscience(all)