RT Journal Article ID 5d48331c019946ce A1 Roth, Bryan L. A1 Berry, Sally A. A1 Kroeze, Wesley K. A1 Willins, David L. A1 Kristiansen, Kurt T1 Serotonin 5-HT2A Receptors: Molecular Biology and Mechanisms of Regulation JF Critical Reviews™ in Neurobiology JO CRN YR 1998 FD 1998-12-01 VO 12 IS 4 SP 319 OP 338 K1 serotonin K1 arrestin K1 protein kinase K1 schizophrenia K1 depression K1 atypical antipsychotic K1 clozapine AB 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. PB Begell House LK https://www.dl.begellhouse.com/journals/7b004699754c9fe6,3458781e2c1a2a0a,5d48331c019946ce.html