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Mu-opioid receptor agonists
Thienorphine
Другие языки:

    Thienorphine

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    Thienorphine
    Thienorphine.svg
    Clinical data
    ATC code
    • None
    Identifiers
    • (1R,2R,6S,15R)-3-(cyclopropylmethyl)-16-[(2R)-2-hydroxy-4-(thiophen-2-yl)butan-2-yl]-15-methoxy-13-oxa-3-azahexacyclo[13.2.2.12,8.01,6.06,14.07,12]icosa-7,9,11-trien-11-ol
    PubChem CID
    ChemSpider
    Chemical and physical data
    Formula C31H39NO4S
    Molar mass 521.72 g·mol−1
    3D model (JSmol)
    • C[C@@](CCc1cccs1)([C@H]2C[C@@]34CCC2([C@H]5[C@@]36CCN([C@@H]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. 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. It also possesses relatively low affinity for the nociceptin receptor (Ki = 36.5 nM), where it acts as an antagonist.

    See also


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