%0 Journal Article %A Roth, Bryan L. %A Berry, Sally A. %A Kroeze, Wesley K. %A Willins, David L. %A Kristiansen, Kurt %D 1998 %I Begell House %K serotonin, arrestin, protein kinase, schizophrenia, depression, atypical antipsychotic, clozapine %N 4 %P 319-338 %R 10.1615/CritRevNeurobiol.v12.i4.30 %T Serotonin 5-HT2A Receptors: Molecular Biology and Mechanisms of Regulation %U https://www.dl.begellhouse.com/journals/7b004699754c9fe6,3458781e2c1a2a0a,5d48331c019946ce.html %V 12 %X 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. %8 1998-12-01