Discovery of 1-[9-(4-Chlorophenyl)-8-(2-chlorophenyl)-9 H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic Acid Amide Hydrochloride (CP-945,598), a Novel, Potent, …

…, PA Carpino, P DaSilva-Jardine, R Day…

Index: Griffith, David A.; Hadcock, John R.; Black, Shawn C.; Iredale, Philip A.; Carpino, Philip A.; Dasilva-Jardine, Paul; Day, Robert; Dibrino, Joseph; Dow, Robert L.; Landis, Margaret S.; O'Connor, Rebecca E.; Scott, Dennis O. Journal of Medicinal Chemistry, 2009 , vol. 52, # 2 p. 234 - 237

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Citation Number: 55

Abstract

We report the structure− activity relationships, design, and synthesis of the novel cannabinoid type 1 (CB1) receptor antagonist 3a (CP-945,598). Compound 3a showed subnanomolar potency at human CB1 receptors in binding (K i= 0.7 nM) and functional assays (K i= 0.12 nM). In vivo, compound 3a reversed cannabinoid agonist-mediated responses, reduced food intake, and increased energy expenditure and fat oxidation in ...