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4418 Thienorphine
5d760ef5b16885378807ddaece9f6934de78597af46175383829ef1895a03a25

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Properties

Chemistry

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.

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