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Emedastine

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Chemical Structure| 87233-61-2 同义名 : -
CAS号 : 87233-61-2
货号 : A634117
分子式 : C17H26N4O
纯度 : 99%
分子量 : 302.414
MDL号 : MFCD00865647
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(396.81 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 100 mg/mL(330.67 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.31mL

0.66mL

0.33mL

16.53mL

3.31mL

1.65mL

33.07mL

6.61mL

3.31mL
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