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Bilastine
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。
Bilastine图片
CAS NO:202189-78-4
包装:1mg
市场价:1176元

产品介绍
Bilastine 是一种选择性组胺 H1 受体拮抗剂,用于治疗过敏性鼻结膜炎和荨麻疹。
Cas No.202189-78-4
别名比拉斯汀
化学名2-(4-(2-(4-(1-(2-ethoxyethyl)-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)ethyl)phenyl)-2-methylpropanoic acid
Canonical SMILESCCOCCN1C2=CC=CC=C2N=C1C(CC3)CCN3CCC4=CC=C(C(C)(C(O)=O)C)C=C4
分子式C28H37N3O3
分子量463.61
溶解度Chloroform: 30 mg/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

Bilastine is a selective histamine H1 receptor antagonist used for treatment of allergic rhinoconjunctivitis and urticaria. Target: Histamine H1 ReceptorBilastine binds to histamine H1-receptors as indicated by its displacement of [3H]-pyrilamine from H1-receptors expressed in guinea-pig cerebellum and human embryonic kidney (HEK) cell lines. The studies conducted on guinea-pig smooth muscle demonstrated the capability of bilastine to antagonise H1-receptors. Bilastine is selective for histamine H1-receptors as shown in receptor-binding screening conducted to determine the binding capacity of bilastine to 30 different receptors [1]. Bilastine distribution has an apparent volume of distribution of 1.29 L/kg, and has an elimination half-life of 14.5 h and plasma protein binding of 84-90% [2].

References:
[1]. Corcostegui, R., et al., Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: receptor selectivity and in vitro antihistaminic activity. Drugs R D, 2005. 6(6): p. 371-84.
[2]. Jauregizar, N., et al., Pharmacokinetic-pharmacodynamic modelling of the antihistaminic (H1) effect of bilastine. Clin Pharmacokinet, 2009. 48(8): p. 543-54.