| 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. Stam, NJ. et al. (1992) European journal of pharmacology 227, 153-62. PMID: 13306472. Cussac, D. et al. (2008) European journal of pharmacology 594, 32-8. PMID: 187030433. Knauer, CS. et al. (2009) Naunyn-Schmiedeberg's archives of pharmacology 379, 461-71. PMID: 190578954. Albizu, L. et al. (2011) Neuropharmacology 61, 770-7. PMID: 216455285. Delille, HK. et al. (2012) Neuropharmacology 62, 2184-91. PMID: 223008366. Cao, D. et al. (2022) Science (New York, N.Y.) 375, 403-411. PMID: 35084960 |
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