MRL-650 (Compound 14; 0.3, 1, or 3 mg/kg)inhibits feeding in a dose-dependent manner. The pharmacokinetic profile of CB1 inverse agonist 1 is evaluated in Sprague-Dawley rats, C57BL/6 mice, beagles, and rhesus macaques with t1/2 of >8, >8, >24, and 22 h, respectively.
参考文献:
1. Debenham JS, et al. Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists.Bioorg Med Chem Lett. 2006 Feb;16(3):681-5.