Thienorphine

This time, we will explore the fascinating world of Thienorphine. From its origins to its impact on today's society, Thienorphine has been the object of study, debate and admiration. Whether through his contributions in a specific field, his influence on popular culture, or his relevance in history, Thienorphine has left an indelible mark on the world. Throughout this article, we will dive into a deep and detailed analysis of Thienorphine, exploring its many facets and offering a new perspective on its importance today. Get ready to discover everything there is to know about Thienorphine!

Thienorphine
Clinical data
ATC code
  • None
Identifiers
  • (1R,2R,6S,15R)-3-(cyclopropylmethyl)-16--15-methoxy-13-oxa-3-azahexacycloicosa-7,9,11-trien-11-ol
PubChem CID
ChemSpider
Chemical and physical data
FormulaC31H39NO4S
Molar mass521.72 g·mol−1
3D model (JSmol)
  • C(CCc1cccs1)(2C34CCC2(536CCN(4Cc7c6c(c(cc7)O)O5)CC8CC8)OC)O
  • InChI=1S/C31H39NO4S/c1-28(34,10-9-21-4-3-15-37-21)23-17-29-11-12-31(23,35-2)27-30(29)13-14-32(18-19-5-6-19)24(29)16-20-7-8-22(33)26(36-27)25(20)30/h3-4,7-8,15,19,23-24,27,33-34H,5-6,9-14,16-18H2,1-2H3/t23-,24-,27-,28-,29-,30+,31-/m1/s1
  • Key:WTGSHWLSWVFVAH-JTTXIWGLSA-N

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

  1. ^ Liu H, Zhong BH, Liu CH, Wu B, Gong ZH (2005). "Synthesis, Crystal Structural and Pharmacological Study of N-Cyclopropylmehtyl-7α-[(R)-1-hydroxyl-1-methyl-3-(thien-2-yl)propyl]-6,14-endoethanotetrahydronooripavine" (PDF). Acta Chimica Slovenica. 52 (1): 80–85. ISSN 1318-0207.
  2. ^ Yu G, Liu YS, Yan LD, Wen Q, Gong ZH (July 2009). "". Yao Xue Xue Bao [Acta Pharmaceutica Sinica] (in Chinese). 44 (7): 726–730. PMID 19806910.
  3. ^ Yu G, Li SH, Cui MX, Yan LD, Yong Z, Zhou PL, et al. (March 2014). "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. doi:10.1111/cns.12210. PMC 6492997. PMID 24330593.
  4. ^ Yu G, Yue YJ, Cui MX, Gong ZH (July 2006). "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. doi:10.1124/jpet.105.099937. PMID 16569757. S2CID 24549788.
  5. ^ Li JX, Becker GL, Traynor JR, Gong ZH, France CP (April 2007). "Thienorphine: receptor binding and behavioral effects in rhesus monkeys". The Journal of Pharmacology and Experimental Therapeutics. 321 (1): 227–236. doi:10.1124/jpet.106.113290. PMID 17220427. S2CID 11477535.
  6. ^ a b Wen Q, Yu G, Li YL, Yan LD, Gong ZH (October 2011). "Pharmacological mechanisms underlying the antinociceptive and tolerance effects of the 6,14-bridged oripavine compound 030418". Acta Pharmacologica Sinica. 32 (10): 1215–1224. doi:10.1038/aps.2011.83. PMC 4010084. PMID 21863064.


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