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Emedastine
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。
Emedastine图片
CAS NO:87233-61-2
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 302.41
Formula C17H26N4O
CAS No. 87233-61-2 (free);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 10 mM
Water: N/A
Ethanol: N/A
Chemical Name 1-(2-Ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidazole
Synonyms AL-3432A; DSSTox_CID_26911; KB 2413; KB-2413; KG 2413; KG-2413; Emadine; Emedastine Difumarate; Emedastine fumarate; Rapimine;
实验参考方法
In Vitro

In vitro activity: Emedastine is a novel, potent, high affinity, selective, second generation H1-receptor antagonist with pre-clinically well-documented anti-allergic effects. Emedastine has Ki value of 1.3 ±0.1 nM for H1-receptors and significantly weaker affinity for H2- (K1 of 49,067 ± 11,113 nM) and H3-receptors (Ki of 12,430 ± 1,282 nM). Emedastine displays pharmacodynamic properties comparable with cetirizine and therefore qualifies as a safe and alternative compound with H1-receptor antagonist properties. Additional larger studies may be needed to substantiate potential benefits of cetirizine over emedastine after single-dose administration.


Kinase Assay: 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). These data yielded ratios of 37744, 9562 and 4 for H2:H1, H3:H1 and H2:H3 receptor affinities, respectively, thus making emedastine a very selective H1-receptor antagonist. 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). Similarly, the respective receptor affinity ratios for ketotifen (858, 1752, 0.5), levocabastine (420, 82, 5), pheniramine (430, 312, 1), chlorpheniramine (5700, 2216, 3) and antazoline (1163, 1110, 1) showed these antihistamines to be also markedly less H1-selective than emedastine. 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. These data indicate emedastine to be a high affinity and high potency histamine antagonist with the highest selectivity for the H1-histamine receptor.


Cell Assay:

In VivoIn Human, following the administration of 4 mg emedastine q.d., mean area under the concentration-time curve (AUC)0-24 values of 34.49 +/- 24.07 ng h ml(-1) and 47.05 +/- 36.12 ng h ml(-1) were attained on day 1 and day 5, respectively. Following the administration of emedastine (2 mg b.i.d.) mean AUC0-24 values were 29.75 +/- 19.92 ng h ml(-1) and 46.13 +/- 38.50 ng h ml(-1) on day 1 and day 5, respectively. Histamine-induced wheals and flares were significantly more effectively suppressed by emedastine and cetirizine than placebo. At pharmacokinetic steady-state levels, no significant difference could be found in the potency between cetirizine and emedastine (2 mg b.i.d.).
Animal model
Formulation & Dosage
References J Ocul Pharmacol. 1994 Winter;10(4):653-64; Eur J Clin Pharmacol. 2000 Feb-Mar;55(11-12):837-41.