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