Lerisetron is an antagonist of serotonin type 3 (5-HT3) receptor, with antiemetic activity.

5-HT3 receptor (cell-free assay):0.81 μM

老年大鼠中，观察到总清除率和中心区室的分布体积有所下降。Lerisetron的自由（未结合）部分在各组间保持不变，且alpha(1)-酸性糖蛋白水平之间无显著差异。浓度-效应关系通过sigmoid E(max)模型进行了最佳描述。由于老年大鼠中Lerisetron在血浆中半最大效应浓度（EC(50)）降低，可预期老年动物对Lerisetron的敏感性增加。

Fischer 344 rats (n = 44) were divided into three groups, depending on their age: 5, 13, and 25 months. Blood samples were collected before administration of 200 micro g/kg of lerisetron for measurements of albumin, alpha(1)-acid glycoprotein, and unbound fraction of lerisetron. The lerisetron plasma concentrations were measured by high-performance liquid chromatography. A two-compartment model was fitted to the data using the nonlinear mixed-effects computer program WinNonMix. The population analysis was performed with the complete set of the collected data, and the potential sources of variability in the population parameters were investigated. Additionally, a pharmacodynamic study was performed. The effect of lerisetron (inhibition of the von Bezold-Jarisch reflex) was evaluated in young, adult, and senescent Fischer 344 rats.