AVN-492

5-HT6受体拮抗剂(Ki=0.09nM)；选择性抑制5-HT6受体而非5-HT2B受体（在放射性配体结合试验中，IC50s分别为0.19和268nM）；抑制表达5-HT6受体的HEK293细胞中5-HT诱导的cAMP水平升高(IC50=1.5nM)；0.2mg/kg剂量可增加大鼠在高架十字迷宫开放臂中停留的时间，表明具有抗焦虑活性；1mg/kg剂量可预防MK-801在被动回避测试中引起的记忆缺陷。An antagonist of the 5-HT6 receptor (Ki = 0.09 nM); selectively inhibits the 5-HT6 receptor over the 5-HT2B receptor (IC50s = 0.19 and 268 nM, respectively, in a radioligand binding assay); inhibits increases in cAMP levels induced by 5-HT in HEK293 cells expressing the 5-HT6 receptor (IC50 = 1.5 nM); increases the time spent in the open arms of the elevated plus maze in rats, indicating anxiolytic activity, at 0.2 mg/kg; prevents memory deficits induced by MK-801 in a passive avoidance test at 1 mg/kg.