| 靶标 | M-OR-1, MOP, MOR-1, MOR1, Mu opiate receptor, Mu opioid receptor, Mu-type opioid receptor, OPRM1, hMOP |
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| 背景 | Mu-type opioid receptor (OPRM1) 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. Zhang, P. et al. (1999) Brain research. Molecular brain research 72, 195-204. PMID: 105294782. Pan, YX. et al. (2003) Biochemical and biophysical research communications 301, 1057-61. PMID: 125898203. Mestek, A. et al. (1995) The Journal of neuroscience : the official journal of the Society for Neuroscience 15, 2396-406. PMID: 78911754. Wang, JB. et al. (1994) FEBS letters 338, 217-22. PMID: 79058395. Bare, LA. et al. (1994) FEBS letters 354, 213-6. PMID: 79579266. Bond, C. et al. (1998) Proceedings of the National Academy of Sciences of the United States of America 95, 9608-13. PMID: 96891287. Law, PY. et al. (2000) Annual review of pharmacology and toxicology 40, 389-430. PMID: 108361428. Lopez, A. et al. (2009) Cellular and molecular life sciences : CMLS 66, 2093-108. PMID: 19300905 |
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