%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