| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T23547 | ||||
| Target Name | Opioid receptor | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | Morphine | Drug Info | IC50 = 12600 nM | [552512] | |
| Levorphanol | Drug Info | Ki = 3.27 nM | [552334] | ||
| Dextropropoxyphene | Drug Info | EC50 = 590 nM | [553204] | ||
| Action against Disease Model | Morphine | Naloxone (10 mg/kg) reduced the analgesic activity of nitrous oxide, ketamine and morphine in the rat tail-flick test. With the exception of pentobarbitone and Althesin, the other anaesthetic agents also induced analgesia but were not antagonized by naloxone.4 Specific [(3)H]-dihydromorphine binding was displaced by the opiates naloxone (IC(50) = 7.6 nm), methionine-enkephalin (Met-enkephalin, IC(50) = 40 nm) and morphine (IC(50) = 54 nm). | [553157] | Drug Info | |
| Methadone | EC50 on isometric twitch tension of isolated papillary muscle of Dunkin-Hartley guinea-pigs: 12500nM | [553249] | Drug Info | ||
| References | |||||
| Ref 552512 | Progress in the discovery of polo-like kinase inhibitors. Curr Top Med Chem. 2005;5(2):181-97. | ||||
| Ref 552334 | Differential regulation of the human kappa opioid receptor by agonists: etorphine and levorphanol reduced dynorphin A- and U50,488H-induced internalization and phosphorylation. J Pharmacol Exp Ther. 2003 May;305(2):531-40. Epub 2003 Jan 24. | ||||
| Ref 553157 | Opiate-like analgesic activity in general anaesthetics. Br J Pharmacol. 1981 Jun;73(2):435-42. | ||||
| Ref 553249 | The mode of action of several opioids on cardiac muscle. Exp Physiol. 1997 Mar;82(2):261-72. | ||||
| Ref 553204 | Interaction between ethanol and opioids in a protozoan assay. Hum Exp Toxicol. 1994 Mar;13(3):145-8. | ||||
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