| 背景 | 5-hydroxytryptamine receptor 2A (HTR2A) is a ~52 kDa protein. G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors. HTR2A is coupled to G(q)/G(11) G alpha proteins and activates phospholipase C-beta, releasing diacylglycerol (DAG) and inositol 1,4,5-trisphosphate (IP3) second messengers that modulate the activity of phosphatidylinositol 3-kinase and promote the release of Ca(2+) ions from intracellular stores, respectively. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. 1. Fiorica-Howells, E. et al. (2002) American journal of physiology. Gastrointestinal and liver physiology 282, G877-93. PMID: 119607842. Weisstaub, NV. et al. (2006) Science (New York, N.Y.) 313, 536-40. PMID: 168736675. Albizu, L. et al. (2011) Neuropharmacology 61, 770-7. PMID: 216455286. Moreno, JL. et al. (2012) The Journal of biological chemistry 287, 44301-19. PMID: 231297627. Nelson, PM. et al. (2012) Experimental diabetes research 2012, 398406. PMID: 23346101 |
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