Epinastine-13C,d3 hydrobromide(Synonyms: WAL801-13C,d3 hydrobromide)

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Epinastine-13C,d3 hydrobromide (Synonyms: WAL801-13C,d3 hydrobromide)

Epinastine-13C,d3 (hydrobromide) 是一种 13C- 和氘代标记的 Epinastine。Epinastine (WAL801) 是一种抗组胺剂和肥大细胞稳定剂。Epinastine 是一种有效的,选择性的,口服活性的组胺 H1 受体 (histamine H1 receptor) 拮抗剂。Epinastine 还抑制 IL-8 释放并具有抗过敏作用。

Epinastine-13C,d3 hydrobromide(Synonyms: WAL801-13C,d3 hydrobromide)

Epinastine-13C,d3 hydrobromide Chemical Structure

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生物活性

Epinastine-13C,d3 (hydrobromide) is the 13C- and deuterium labeled. Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action[1][2][3][4].

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[68].

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

分子量

334.23

Formula

C1513CH13D3BrN3

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]. Fugner, A., et al., In vitro and in vivo studies of the non-sedating antihistamine epinastine. Arzneimittelforschung, 1988. 38(10): p. 1446-53.

    [3]. Roeder, T., J. Degen, and M. Gewecke, Epinastine, a highly specific antagonist of insect neuronal octopamine receptors. Eur J Pharmacol, 1998. 349(2-3): p. 171-7.

    [4]. Kamei, C., et al., Antiallergic effect of epinastine (WAL 801 CL) on immediate hypersensitivity reactions: (I). Elucidation of the mechanism for histamine release inhibition. Immunopharmacol Immunotoxicol, 1992. 14(1-2): p. 191-205.

    [5]. Kohyama, T., et al., A novel antiallergic drug epinastine inhibits IL-8 release from human eosinophils. Biochem Biophys Res Commun, 1997. 230(1): p. 125-8.

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