CB1 inverse agonist 1

CB1 inverse agonist 1 is a highly potent, orally active, and specific inverse agonist of CB1 receptor with IC50s of 7.5 nM and 4100 nM for CB1 and CB2 receptors, respectively. Anorexigenic effects[1].

Research Areas >> Metabolic Disease

Signaling Pathways >> GPCR/G Protein >> Cannabinoid Receptor

CB1:7.5 nM (IC50)

CB2:4100 nM (IC50)

CB1 inverse agonist 1 (Compound 14; 0.3, 1, or 3 mg/kg）inhibits feeding in a dose-dependent manner[1]. 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[1]. Animal Model: Rat[1] Dosage: 0.3, 1, or 3 mg/kg Administration: PO Result: Inhibited feeding in a dose-dependent manner. 3 mg/kg decreased cumulative food intake from 2 h post-dosing. Decreased overnight body weight gain compared to vehicle treatment at all dosing levels.

[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.