U50488

U50488 is a highly selective, synthetic κ-opioid receptor agonist with no significant μ-opioid antagonism. It exhibits potent analgesic, diuretic, and antitussive effects in preclinical studies, and has also been shown experimentally to reverse memory impairment caused by anticholinergic drugs. U50488 and its hydrochloride salt (U-50488H) were among the first non-peptide kappa agonists developed for scientific research, and their pharmacology led to the design of related selective kappa agonists. U50488 is also a kappa-opioid receptor agonist with mild calcium channel blocking activity. It does not cause physical dependence, but tolerance develops with chronic administration. U50488 has not been FDA approved, is not used in humans, and remains a research tool for the study of opioid receptor pharmacology.[1][3][8]

Other names

3,4-dichloro-n-methyl-n-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamidetrans-3,4-Dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]-benzeneacetamideCAS 67198-13-4CAS67198-13-4CAS-67198-13-4