生物活性
Azatadine (SCH10649) 是一种抗组胺和抗胆碱能药物，IC50分别为6.5nM和10nM。
靶点
TargetValue
Histamine receptor
6.5 nM
Cholinergic
10 nM
95% Azatadine在Sabouraud葡萄糖肉汤中72小时内生物转化为两个主要代谢物，7-hydroxyazatadine (25%)和8-hydroxyazatadine (50%)，和两个次要代谢物，N-desmethylazatadine和9-hydroxyazatadine。
体内研究
在有意识的豚鼠体内，Azatadine延迟雾化组胺，乙酰胆碱和血清素诱导的呼吸困难的发生，PD50 为0.01 mg/kg，0.739 mg/kg 和 0.86 mg/kg。Azatadine对静脉注射组胺诱导的死亡产生保护作用，在有意识的豚鼠和小鼠体内口服PD50分别为0.009 mg/kg和0.22 mg/kg。在禁食的志愿者中，Azatadine (4 mg)单剂量口服给药4.2小时后，RIA 4.2测量表明C
为3 μg/L。Azatadine几乎通过羟基化，脱甲基化，以及氧化环打开后zwitterion异构体的形成完全代谢。Azatadine (8.8 mg口服)治疗5.3小时后在健康志愿者中的Csub max为5.9 μg/L，生物利用度为80%。 Azatadine (1 mg每天两次，14天)能够有效减轻组胺介导的季节性过敏鼻炎的症状。
化夏化学
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14604
6,11-Dihydro-11-(1-methyl-4-piperidylidene)5H-benzo(5,6)cyclohepta(1,2-B)pyridine dimaleate
5H-Benzo(5,6)cyclohepta(1,2-B)pyridine, 6,11-dihydro-11-(1-methyl-4-piperidinylidene)-, (Z)-2-butenedioate (1:2)
11H-Benzo(5,6)cyclohepta(1,2-B)pyridine, 5,6-dihydro-11-(1-methyl-4-piperidylidene)-, dimaleate
6,11-dihydro-11-(1-methylpiperidin-4-ylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine dimaleate
AZATADINE MALEATE (200 MG)
sch10649
optimine
idulian
idinedimaleate
azatadinemaleate
Azatadine Maleate(Azatadine dimaleate)
5H-Benzo[5,6]cyclohepta[1,2-b]pyridine, 6,11-dihydro-11-(1-methyl-4-piperidinylidene)-, (2Z)-2-butenedioate (1:2)
azatadinedimaleate
6,11-dihydro-11-(1-methyl-4-piperidylidene)5h-benzo(5,6)cyclohepta(1,2-b)pyr
11h-benzo(5,6)cyclohepta(1,2-b)pyridine,5,6-dihydro-11-(1-methyl-4-piperidylid
Zadine
AZATADINE MALEATE;OPTIMINE;ZADINE
