Azatadine (maleate)

一种具有抗胆碱能和抗血清素活性的抗组胺药；组胺H1受体拮抗剂（Ki=3.9nM）；抑制组胺和乙酰胆碱引起的豚鼠髂骨收缩以及5-HT引起的大鼠子宫收缩（EC50s分别为6.5、10和14nM）；延迟豚鼠气雾化组胺、5-HT或乙酰胆碱引起的呼吸困难的发作；预防组胺引起的豚鼠致死和小鼠爪水肿（ED50s分别为9和68μg/kg）；提高豚鼠和小鼠过敏性休克模型的存活率（PD50s分别为0.024和0.019mg/kg）。An antihistamine with anticholinergic and antiserotonergic activities; histamine H1 receptor antagonist (Ki = 3.9 nM); inhibits histamine- and acetylcholine-induced contractions in isolated guinea pig ilium and 5-HT-induced contractions in isolated rat uterus (EC50s = 6.5, 10, and 14 nM, respectively); delays the onset of dyspnea induced by aerosolized histamine, 5-HT, or acetylcholine in guinea pigs; prevents histamine-induced lethality in guinea pigs and paw edema in mice (ED50s = 9 and 68 μg/kg, respectively); increases survival in guinea pig and mouse models of anaphylactic shock (PD50s = 0.024 and 0.019 mg/kg, respectively).