Target Validation Information
TTD ID	T23547
Target Name	Opioid receptor (OPR)
Type of Target	Successful
Drug Potency against Target	Dextropropoxyphene	Drug Info	EC50 = 590 nM	[4]
	Levorphanol	Drug Info	Ki = 3.27 nM	[1]
	Morphine	Drug Info	IC50 = 12600 nM	[2]
Action against Disease Model	Methadone	Drug Info	EC50 on isometric twitch tension of isolated papillary muscle of Dunkin-Hartley guinea-pigs: 12500nM	[5]
	Morphine	Drug Info	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).	[3]
References
REF 1	Differential regulation of the human kappa opioid receptor by agonists: etorphine and levorphanol reduced dynorphin A- and U50,488H-induced interna... J Pharmacol Exp Ther. 2003 May;305(2):531-40.
REF 2	Progress in the discovery of polo-like kinase inhibitors. Curr Top Med Chem. 2005;5(2):181-97.
REF 3	Opiate-like analgesic activity in general anaesthetics. Br J Pharmacol. 1981 Jun;73(2):435-42.
REF 4	Interaction between ethanol and opioids in a protozoan assay. Hum Exp Toxicol. 1994 Mar;13(3):145-8.
REF 5	The mode of action of several opioids on cardiac muscle. Exp Physiol. 1997 Mar;82(2):261-72.

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