Taranabant (MK-0364) is a potent, selective and orally active cannabinoid-1 receptor (CB1R) inverse agonist with IC50 of 2.8 nM, Ki of 0.13 nM.
Taranabant displays >1000-fold selectivity over CB2R (Ki=170 nM), AT1R, NK2R, A3R, MT1R, D1R, etc.
Taranabant dose-dependently inhibits food intake and weight gain in diet-induced obese (DIO) rats with an acute minimum effective dose of 1 mg/kg and has good pharmacokinetic.
