【文章名】Discovery of 1-[9-(4-Chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopip eridine-4-carboxylic Acid Amide Hydrochloride (CP-945,598), a Novel, Potent, and Selective Cannabinoid Type 1 Receptor Antagonist.
Discovery of 1-[9-(4-Chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopip eridine-4-carboxylic Acid Amide Hydrochloride (CP-945,598), a Novel, Potent, and Selective Cannabinoid Type 1 Receptor Antagonist.
作者
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.;
[摘要]：We report the structure-activity relationships, design, and synthesis of the novel cannabinoid type 1 (CB1) receptor antagonist 3a (CP-945,598). Compd. 3a (I) showed subnanomolar potency at human CB1 receptors in binding (Ki = 0.7 nM) and functional assays (Ki = 0.12 nM). In vivo, compd. 3a reversed cannabinoid agonist-mediated responses, reduced food intake, and increased energy expenditure and fat oxidn. in rodents.
