Chemistry:Thienorphine
From HandWiki
Short description: Chemical compound
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| Formula | C31H39NO4S |
| Molar mass | 521.72 g·mol−1 |
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Thienorphine is a very potent, extremely long-acting, orally-active opioid analgesic with mixed agonist–antagonist properties which was developed by the Beijing Institute of Pharmacology and Toxicology as a potential treatment for opioid dependence.[1][2][3] It is a high-affinity, balanced ligand of the μ- (Ki = 0.22 nM), δ- (Ki = 0.69 nM), and κ-opioid receptors (Ki = 0.14 nM), behaving as a partial agonist of the μ- (Emax = 19%–28%) and κ-opioid receptors (Emax = 65–75%) and as an antagonist of the δ-opioid receptor.[4][5][6] It also possesses relatively low affinity for the nociceptin receptor (Ki = 36.5 nM), where it acts as an antagonist.[6]
See also
References
- ↑ "Synthesis, Crystal Structural and Pharmacological Study of N-Cyclopropylmehtyl-7α-[(R)-1-hydroxyl-1-methyl-3-(thien-2-yl)propyl-6,14-endoethanotetrahydronooripavine"]. Acta Chimica Slovenica 52 (1): 80–85. 2005. ISSN 1318-0207. http://acta-arhiv.chem-soc.si/52/52-1-80.pdf.
- ↑ "[Structure-activity relationships analysis of thienorphine and its derivatives]" (in zh). Yao Xue Xue Bao 44 (7): 726–730. July 2009. PMID 19806910.
- ↑ "Multiple mechanisms underlying the long duration of action of thienorphine, a novel partial opioid agonist for the treatment of addiction". CNS Neuroscience & Therapeutics 20 (3): 282–288. March 2014. doi:10.1111/cns.12210. PMID 24330593.
- ↑ "Thienorphine is a potent long-acting partial opioid agonist: a comparative study with buprenorphine". The Journal of Pharmacology and Experimental Therapeutics 318 (1): 282–287. July 2006. doi:10.1124/jpet.105.099937. PMID 16569757.
- ↑ "Thienorphine: receptor binding and behavioral effects in rhesus monkeys". The Journal of Pharmacology and Experimental Therapeutics 321 (1): 227–236. April 2007. doi:10.1124/jpet.106.113290. PMID 17220427.
- ↑ 6.0 6.1 "Pharmacological mechanisms underlying the antinociceptive and tolerance effects of the 6,14-bridged oripavine compound 030418". Acta Pharmacologica Sinica 32 (10): 1215–1224. October 2011. doi:10.1038/aps.2011.83. PMID 21863064.
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