| Fondo | Mu-type opioid receptor (OPRM1/μOR) is a ~44 kDa protein. Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone. Also activated by enkephalin peptides, such as Met-enkephalin or Met-enkephalin-Arg-Phe, with higher affinity for Met-enkephalin-Arg-Phe. Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociation of the G-protein complex with the free GTP-bound G-protein alpha and the G-protein beta-gamma dimer activating downstream cellular effectors. The agonist- and cell type-specific activity is predominantly coupled to pertussis toxin-sensitive G(i) and G(o) G alpha proteins, GNAI1, GNAI2, GNAI3 and GNAO1 isoforms Alpha-1 and Alpha-2, and to a lesser extent to pertussis toxin-insensitive G alpha proteins GNAZ and GNA15. 1. George, SR. et al. (2000) The Journal of biological chemistry 275, 26128-35. PMID: 108421672. Rios, C. et al. (2006) British journal of pharmacology 148, 387-95. PMID: 166829643. Milan-Lobo, L. et al. (2011) The Journal of pharmacology and experimental therapeutics 337, 868-75. PMID: 214221646. Kaufman, DL. et al. (1995) The Journal of biological chemistry 270, 15877-83. PMID: 77975937. Sora, I. et al. (1997) Proceedings of the National Academy of Sciences of the United States of America 94, 1544-9. PMID: 90370908. Trieu, BH. et al. (2022) Science (New York, N.Y.) 375, 1177-1182. PMID: 35201898 |
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