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Croston, Glenn E; Olsson, Roger; Currier, Erika A; Burstein, Ethan S; Weiner, David; Nash, Norman; Severance, Daniel; Allenmark, Stig G; Thunberg, Linda; Ma, Jian-Nong; Mohell, Nina; O'Dowd, Brian; Brann, Mark R; Hacksell, Uli
Journal of medicinal chemistry, 11/2002, Letnik: 45, Številka: 23Journal Article
A functional cell-based screen identified 3-(4-chlorophenyl)-3-(2-(dimethylamino)ethyl)isochroman-1-one hydrochloride (AC-7954, 1) as a nonpeptidic agonist of the urotensin-II receptor. Racemic 1 had an EC50 of 300 nM at the human UII receptor and was highly selective. Testing of the enantiopure (+)- and (−)- 1 revealed that the UII receptor activity of racemic 1 resides primarily in (+)-1. Being a selective nonpeptidic druglike UII receptor agonist, (+)-1 will be useful as a pharmacological research tool and a potential drug lead.
