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ATC code |
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PubChem CID | |
ChemSpider | |
Chemical and physical data | |
Formula | C31H39NO4S |
Molar mass | 521.72 g·mol−1 |
3D model ( JSmol) | |
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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]
Clinical data | |
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ATC code |
|
Identifiers | |
| |
PubChem CID | |
ChemSpider | |
Chemical and physical data | |
Formula | C31H39NO4S |
Molar mass | 521.72 g·mol−1 |
3D model ( JSmol) | |
| |
|
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]