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Ebastine
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。
Ebastine图片
CAS NO:90729-43-4
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
50mg电议

产品介绍
Ebastine (LAS-W 090) 是一种口服有效的第二代组胺 H1 受体拮抗剂。
Cas No.90729-43-4
别名依巴斯汀; LAS-W 090; RP64305
化学名4-(4-benzhydryloxypiperidin-1-yl)-1-(4-tert-butylphenyl)butan-1-one
Canonical SMILESCC(C)(C)C1=CC=C(C=C1)C(=O)CCCN2CCC(CC2)OC(C3=CC=CC=C3)C4=CC=CC=C4
分子式C32H39NO2
分子量469.66
溶解度≥ 16.6mg/mL in Ethanol
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

Ebastine(LAS-W 090;RP64305) is a long-acting and selective H1-histamine receptor antagonist.Target: Histamine H1 ReceptorEbastine is a H1 antihistamine with low potential for causing drowsiness. Ebastine (10 mg orally) causes brain histamine H1-receptor occupation of approximately 10%, consistent with its lower incidence of sedative effect, whereas (+)-chlorpheniramine occupied about 50% of brain H1-receptors even at a low but sedative dose of 2 mg; occupancy of (+)-chlorpheniramine was correlated with plasma (+)-chlorpheniramine concentration [1]. ebastine 10 or 20 mg once daily was rapidly effective in relieving symptoms of PAR in adult and adolescent patients; additional benefits of the 20-mg dose became apparent in the longer term [2]. ebastine is an effective and generally well-tolerated treatment for allergic rhinitis and chronic idiopathic urticaria. In addition to the regular tablet formulation, ebastine is available as a FDT, providing a treatment option that is particularly convenient for patients [3].

References:
[1]. Tagawa, M., et al., Neuroimaging of histamine H1-receptor occupancy in human brain by positron emission tomography (PET): a comparative study of ebastine, a second-generation antihistamine, and (+)-chlorpheniramine, a classical antihistamine. Br J Clin Pharmacol, 2001. 52(5): p. 501-9.
[2]. Bousquet, J., et al., A 12-week, placebo-controlled study of the efficacy and safety of ebastine, 10 and 20 mg once daily, in the treatment of perennial allergic rhinitis. Multicentre Study Group. Allergy, 1999. 54(6): p. 562-8.
[3]. Sastre, J., Ebastine in allergic rhinitis and chronic idiopathic urticaria. Allergy, 2008. 63 Suppl 89: p. 1-20.