Where Structure Meets Function

摘要: 5-Hydroxytryptamine 2 (serotonin , 5-HT )-family receptors are important for mediating many physiological functions, including vascular and nonvascular smooth muscle contraction, platelet aggregation, modulation of perception, mood, anxiety, feeding behavior. A large number psychopharmaceuticals, atypical antipsychotic drugs, antidepressants, anxiolytics, hallucinogens, mediate their actions, at least in part, via interactions with various -family receptors. This review article summarizes information about structure-function aspects Evidence is presented that implies conserved aromatic charged residues essential ligand binding to 2A Additionally, findings reviewed consistent the hypothesis located intracellular loops 3 (i2 i3) coupling specific G a -subunits such as q . Studies suggest may be down-regulated by both agonists antagonists, usually this down-regulation due post-transcriptional mechanisms. Finally, model regulation receptor-mediated endocytosis advanced, particular structural features responsible endocytotic pathways emphasized. Taken together, these results discrete domains receptor structure binding, G-protein coupling, internalization. pharmacol. ther 79(3):231–257, 1998. © 1998 Elsevier Science Inc.