Discovery of 1-[9-(4-Chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic Acid Amide Hydrochloride (CP-945,598), a Novel, Potent, and Selective Cannabinoid Type 1 Receptor Antagonist
Journal of Medicinal Chemistry2008Vol. 52(2), pp. 234–237
Citations Over TimeTop 10% of 2008 papers
David A. Griffith, John R. Hadcock, Shawn C. Black, Philip A. Iredale, Philip A. Carpino, Paul DaSilva‐Jardine, Robert F. Day, Joseph DiBrino, Robert L. Dow, Margaret S. Landis, Rebecca E. O’Connor, Dennis O. Scott
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 (Ki = 0.7 nM) and functional assays (Ki = 0.12 nM). In vivo, compound 3a reversed cannabinoid agonist-mediated responses, reduced food intake, and increased energy expenditure and fat oxidation in rodents.
Related Papers
- → Inhibition of methamphetamine self-administration in rats by cannabinoid receptor antagonist AM 251(2002)79 cited
- → Pharmacological profiling of the hemodynamic effects of cannabinoid ligands: a combined in vitro and in vivo approach(2015)24 cited
- → New Pyridone-Based Derivatives as Cannabinoid Receptor Type 2 Agonists(2021)11 cited
- → Cannabinoid CB 1 -mediated inhibition of stress-induced gastric ulcers in rats(2001)56 cited