title: Serotonin 5-HT2A receptors: molecular biology and mechanisms of regulation.
abstract: Serotonin 5-HT2A receptors are essential for a large number of physiological functions in the central nervous system and periphery. This review article summarizes our current knowledge of the molecular biology and mechanisms of regulation of 5-HT2A receptors. The mode of drug binding using data derived from molecular modeling and site-directed mutagenesis is described. The cellular and subcellular localization of 5-HT2A receptors is described, and the concentration of 5-HT2A receptors on apical dendrites of pyramidal neurons is emphasized. Various modes of regulation of 5-HT2A receptors are also summarized, including transcriptional, post-translational and mRNA editing processes. Finally, an integrated model of 5-HT2A receptor regulation that involves various protein kinases (protein kinase C, G-protein receptor kinases), arrestins, clathrin-coated vesicles, endosomes and lysosomes. The relevance of these pathways for antidepressant and antipsychotic drug actions is emphasized.
authors.affiliation: Department of Psychiatry, Case Western Reserve University Medical School, Cleveland, OH 44106, USA.
authors.forename: B L
authors.initials: BL
authors.lastname: Roth
authors.forename: S A
authors.initials: SA
authors.lastname: Berry
authors.forename: W K
authors.initials: WK
authors.lastname: Kroeze
authors.forename: D L
authors.initials: DL
authors.lastname: Willins
authors.forename: K
authors.initials: K
authors.lastname: Kristiansen
mesh_terms: D000818:Animals; D003863:Depression / Q000209:etiology; D006801:Humans; D011494:Protein Kinases / Q000494:pharmacology; D011985:Receptors, Serotonin / Q000737:chemistry / Q000187:drug effects / Q000502:physiology*; D012559:Schizophrenia / Q000209:etiology; D018490:Serotonin Agents / Q000494:pharmacology; D014157:Transcription Factors / Q000096:biosynthesis / Q000187:drug effects
chemical_list: D011985:Receptors, Serotonin; D018490:Serotonin Agents; D014157:Transcription Factors; D011494:Protein Kinases