Thienorphine Explained

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- (K_i = 0.22 nM), δ- (K_i = 0.69 nM), and κ-opioid receptors (K_i = 0.14 nM), behaving as a partial agonist of the μ- (E_max = 19%–28%) and κ-opioid receptors (E_max = 65–75%) and as an antagonist of the δ-opioid receptor.^{[4] [5] [6]} It also possesses relatively low affinity for the nociceptin receptor (K_i = 36.5 nM), where it acts as an antagonist.

See also

• Buprenorphine
• Etorphine
• Dihydroetorphine
• Diprenorphine

Notes and References

1. Liu H, Zhong BH, Liu CH, Wu B, Gong ZH . 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 . 2005 . 52 . 1 . 80–85 . 1318-0207.
2. Yu G, Liu YS, Yan LD, Wen Q, Gong ZH . [Structure-activity relationships analysis of thienorphine and its derivatives] . zh . Yao Xue Xue Bao . Acta Pharmaceutica Sinica . 44 . 7 . 726–730 . July 2009 . 19806910 .
3. Yu G, Li SH, Cui MX, Yan LD, Yong Z, Zhou PL, Su RB, Gong ZH . 6 . 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 . 24330593 . 6492997 . 10.1111/cns.12210 .
4. Yu G, Yue YJ, Cui MX, Gong ZH . 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 . 16569757 . 10.1124/jpet.105.099937 . 24549788 .
5. Li JX, Becker GL, Traynor JR, Gong ZH, France CP . Thienorphine: receptor binding and behavioral effects in rhesus monkeys . The Journal of Pharmacology and Experimental Therapeutics . 321 . 1 . 227–236 . April 2007 . 17220427 . 10.1124/jpet.106.113290 . 11477535 .
6. Wen Q, Yu G, Li YL, Yan LD, Gong ZH . 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 . 21863064 . 4010084 . 10.1038/aps.2011.83 .