GR159897

非肽类NK2受体拮抗剂；与NK2受体结合（Ki=0.32nM）；在放射性配体结合试验中，对NK2受体的选择性优于NK1和NK3受体（Kis分别为5,010和>1,000nM）；抑制GR64349引起的豚鼠离体气管收缩（pA2=8.7）；在0.12mg/kg剂量下抑制GR64349引起的麻醉豚鼠支气管收缩；在0.2-50µg/kg剂量下，增加狨猴在与人类观察者对峙时在笼子前面停留的时间。A nonpeptide NK2 receptor antagonist; binds to NK2 receptors (Ki = 0.32 nM); selective for NK2 over NK1 and NK3 receptors in radioligand binding assays (Kis = 5,010 and >1,000 nM, respectively); inhibits GR64349-induced contractions in isolated guinea pig trachea (pA2 = 8.7); inhibits GR64349-induced bronchoconstriction in anesthetized guinea pigs at 0.12 mg/kg; increases the amount of time spent in the front of the cage during confrontation with a human observer in marmosets from 0.2-50 µg/kg.分子式C23H27FN2O2S分子量414.5O=[S@@](C1=CC=CC=C1)CC(OC)(CC2)CCN2CCC(C3=C4)=CNC3=CC=C4F