Emedastine-13C,d3 fumarate

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Emedastine-13C,d3 fumarate 

Emedastine-13C,d3 (fumarate) 是一种 13C- 和氘代标记的 Emedastine。Emedastine 是一种具有口服活性,选择性和高亲和力的组胺 H1 受体拮抗剂,Ki 值为 1.3 nM。Emedastine 是一种苯并咪唑衍生物,具有强大的抗过敏特性,可用于过敏性鼻炎,过敏性皮肤疾病和过敏性结膜炎。

Emedastine-13C,d3 fumarate

Emedastine-13C,d3 fumarate Chemical Structure

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生物活性

Emedastine-13C,d3 (fumarate) is the 13C- and deuterium labeled. Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis[1][2][3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[67].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

422.50

Formula

C2013CH27D3N4O5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-223.

    [2]. Sharif NA, et al. Emedastine: a potent, high affinity histamine H1-receptor-selective antagonist for ocular use: receptor binding and second messenger studies. J Ocul Pharmacol. 1994 Winter;10(4):653-64.

    [3]. Murota H, et al. Emedastine difumarate: a review of its potential ameliorating effect for tissue remodeling in allergic diseases. Expert Opin Pharmacother. 2009 Aug;10(11):1859-67.

    [4]. Andoh T, et al. Involvement of blockade of leukotriene B(4) action in anti-pruritic effects of emedastine in mice. Eur J Pharmacol. 2000 Oct 6;406(1):149-52.

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