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Azatadine dimaleate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Azatadine dimaleate图片
CAS NO:3978-86-7
包装与价格:
包装价格(元)
5mg电议
20mg电议

产品介绍
Azatadine dimaleate 是一种组胺和胆碱能抑制剂,IC50 分别为 6.5 nM 和 10 nM。
Cas No.3978-86-7
别名马来酸阿扎他定; Azatadine maleate
化学名(Z)-but-2-enedioic acid;11-(1-methylpiperidin-4-ylidene)-5,6-dihydrobenzo[1,2]cyclohepta[3,4-b]pyridine
Canonical SMILESCN1CCC(=C2C3=CC=CC=C3CCC4=C2N=CC=C4)CC1.C(=CC(=O)O)C(=O)O.C(=CC(=O)O)C(=O)O
分子式C28H30N2O8
分子量522.55
溶解度DMF: 20mg/mL,DMSO: 20mg/mL,Ethanol: 5mg/mL,PBS (pH 7.2): 10mg/mL
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Azatadine dimaleate is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.Target: Histamine ReceptorAzatadine, a new antihistamine, was evaluated for its efficacy in 20 patients with chronic allergic rhinitis. Eighty percent of patients had symptomatic relief with a twice daily dosage of 2 mg. Sedation was volunteered as a side effect by six of the patients and was admitted by two further patients after specific questioning. A choice reaction time test gave slowing of motor function in these sedated patients. Four of the previously sedated patients experienced good symptomatic control with minimal sedation when the azatadine dose was reduced to 1 mg twice daily; slowing of motor function was not observed at this, the normal recommended dose.Azatadine delays the onset of dyspnea-induced by aerosolized histamine, acetylcholine and serotonin in the conscious guinea-pig with PD50 of 0.01 mg/kg, 0.739 mg/kg and 0.86 mg/kg. Azatadine protects conscious guinea-pigs against death induced by the intravenous injection of histamine with oral PD50 of 0.009 mg/kg in guinea-pig and 0.22 mg/kg in mice.

References:
[1]. Wilson JD, et al. Azatadine maleate (Zadine): evaluation in the management of allergic rhinitis. N Z Med J. 1981 Aug 12;94(689):79-81.
[2]. Tozzi S, et al. The pharmacology of azatadine, a potential antiallergy drug. Agents Actions. 1974 Oct;4(4):264-70.