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Critical Reviews™ in Neurobiology

ISSN Print: 0892-0915
ISSN Online: 2375-0014

Archives: Volume 10, 1996 to Volume 20, 2008

Critical Reviews™ in Neurobiology

DOI: 10.1615/CritRevNeurobiol.v12.i4.30
pages 319-338

Serotonin 5-HT2A Receptors: Molecular Biology and Mechanisms of Regulation

Bryan L. Roth
Departments of Biochemistry, Psychiatry and Neurosciences and National Institute of Mental Health Psychoactive Drug Screening Program. Case Western Reserve University Medical School, Cleveland, Ohio, USA
Sally A. Berry
Department of Psychiatry, Case Western Reserve University Medical School, Cleveland, OH 44106
Wesley K. Kroeze
Department of Biochemistry, Case Western Reserve University Medical School, Cleveland, OH 44106
David L. Willins
Department Biochemistry, Case Western Reserve University Medical School, Cleveland, OH 44106
Kurt Kristiansen
Department Biochemistry, Case Western Reserve University Medical School, Cleveland, OH 44106; Current Address: Royal Danish School of Pharmacy, Department of Medicinal Chemistry, Copenhagen, Denmark

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.


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