Taranabant

CB1受体反向激动剂(Ki=0.13nM)；对CB1受体的选择性优于CB2受体(Ki=170nM)，并且1µM浓度下可作用于170种受体、酶、离子通道和转运蛋白；增加表达人CB1的CHO细胞膜中福斯高林诱导的cAMP生成(EC50=2nM)；在3mg/kg剂量下逆转由CB受体激动剂CP55,940引起的大鼠低温；在1mg/kg和3mg/kg剂量下可减少野生型小鼠（但CB1受体缺陷型小鼠）两小时和过夜食物摄入量以及过夜体重增加A CB1 receptor inverse agonist (Ki = 0.13 nM); selective for CB1 over CB2 receptors (Ki = 170 nM), as well as a panel of 170 receptors, enzymes, ion channels, and transporters at 1 µM; increases forskolin-induced cAMP production in CHO cell membranes expressing human CB1 (EC50 = 2 nM); reverses hypothermia induced by the CB receptor agonist CP 55,940 in rats at 3 mg/kg; reduces two-hour and overnight food intake, as well as overnight weight gain in wild-type, but not CB1 receptor-deficient, mice at 1 and 3 mg/kg.