Pitolisant hydrochloride (Ciproxidine) is a potent and selective inverse agonist of the histamine H3 receptor(Ki : 0.16 nM).

H3 receptor:0.16 nM(ki)

在高脂肪饮食下喂养的小鼠，在12周的肥胖诱导期间体重增加更多。同时摄入高脂肪饮食并在接下来的14天内接受pitolisant治疗的动物，其体重增加明显少于控制组摄入高脂肪饮食的小鼠。从pitolisant给药的第10天起，两组间体重的差异统计上显著。MeTheaflavinormin作为正向对照，从给药第九天开始减轻体重[1]。

Male CD-1 mice were fed on high-fat diet consisting of 40% fat blend (Labofeed B with 40% lard) for 14 weeks, water and 30% sucrose available ad libitum. Control mice were fed on a standard diet and drank water only. After 12 weeks, mice with obesity induced via their diet were randomly divided into three equal groups that had the same mean body weight and were treated intraperitoneally with test compounds at the following doses: pitolisant 10 mg/kg bw/day or metformin 100 mg/kg bw/day; control group: vehicle =1% Tween 80, 0.35 ml/kg (high-fat/sugar diet + vehicle = obesity control group) once daily in the morning, between 9:00 and 10:00 AM for 14 days. Control mice (control without obesity) were maintained on a standard diet, with intraperitoneal administration of vehicle = 1% Tween 80, 0.35 ml/kg (standard diet + vehicle = control group). Water and sucrose were measured daily, immediately prior to administration of drugs. Animals always had free access to feed, water and sucrose[1].