87233-61-2|Emedastine|CsnPharm

CAS No.: 87233-61-2

Emedastine/依美斯汀 Catalog No. CSN24500

Synonyms: 依美斯汀

Emedastine is a potent, high affinity histamine H1-receptor-selective antagonist with Ki of 1.3 ±0.1 nM for H1-receptors while considerably weaker at H2- (Ki = 49,067 ± 11,113 nM) and H3-receptors (Ki = 12,430 ± 1,282 nM).

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技术信息

生物活性

描述Emedastine is a high affinity and high potency histamine antagonist with the highest selectivity for the H1-histamine receptor. Emedastine exhibited the highest affinity for H1-receptors (dissociation constant, Ki = 1.3 +/- 0.1 nM), and was considerably weaker at H2- (K1 = 49,067 +/- 11,113 nM) and H3-receptors (Ki = 12,430 +/- 1,282 nM). The H1-selectivity of emedastine was considerably superior to that of pyrilamine (H2:H1, H3:H1 and H2:H3 ratios of 11887, 12709 and 1, respectively). The potency of emedastine (IC50 = 1.44 +/- 0.3 nM) for antagonizing histamine-induced phosphoinositide turnover in human trabecular meshwork cells compared well with its binding affinity at the H1-receptor^[1]. Emedastine displays pharmacodynamic properties comparable with cetirizine and therefore qualifies as a safe and alternative compound with H1-receptor antagonist properties^[2]. In the Vienna Challenge Chamber model, ketotifen and emedastine both effectively alleviated ocular symptoms of SAC (seasonal allergic conjunctivitis) after single-dose administration^[3].
参考文献

[1] Sharif NA, Su SX, Yanni JM. 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
[2] Jansen B, Graselli U, Dallinger S, Kiss B, Wacheck V, Schlagbauer-Wadl H, Assandri A, Müller M. Pharmacokinetics and pharmacodynamics of the novel H1-receptor antagonist emedastine in healthy volunteers. Eur J Clin Pharmacol. 2000 Feb-Mar;55(11-12):837-41
[3] Horak F, Stübner P, Zieglmayer R, Kawina A, Moser M, Lanz R. Onset and duration of action of ketotifen 0.025% and emedastine 0.05% in seasonal allergic conjunctivitis : efficacy after repeated pollen challenges in the vienna challenge chamber. Clin Drug Investig. 2003;23(5):329-37

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.3067 mL
- 16.5336 mL
- 33.0672 mL
- 5 mM
- 0.6613 mL
- 3.3067 mL
- 6.6134 mL
- 10 mM
- 0.3307 mL
- 1.6534 mL
- 3.3067 mL

技术信息

CAS号

87233-61-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H26N4O

运输

蓝冰

分子量

302.41

别名

依美斯汀

溶解度

DMSO	540.0 mg/mL (1785.6 mM)
Water	360.0 mg/mL (1190.4 mM)

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