Emedastine (fumarate)
(Synonyms:富马酸依美斯汀;Emedastine Difumarate 富马酸依美斯汀;二福马酸依美斯汀;二富马酸依美斯汀;富马酸伊美斯汀EMEDASTINE DIFUMARATE;富马酸依美斯汀 EP标准品;富马酸依美斯汀 USP标准品;富马酸依美斯汀标准品;甲苯-2,5-二胺;依美斯汀富马酸盐;1-(2-乙氧基乙基)-2-(4-甲基-1-哌嗪基)苯并咪唑富马酸盐;依美斯汀二富马酸盐)
目录号 : KCM15544
CAS No. : 87233-62-3
纯度 : ≥98%
Emedastine is a histamine H receptor antagonist (K = 1.3 nM). It is selective for histamine H over H and H receptors (Ks = 49 and 12.43 µM, respectively), as well as α-, α-, and β-adrenergic and dopamine D1 and D receptors, and the serotonin (5-HT) receptor subtypes 5-HT and 5-HT at 10 µM. Emedastine inhibits histamine-induced phosphoinositide turnover and intracellular calcium mobilization in primary human conjunctival epithelial cells (HCECs; ICs = 1.6 and 2.9 nM, respectively). It also inhibits histamine-stimulated secretion of IL-6, IL-8, and GM-CSF by primary HCECs (ICs = 2.23, 3.42, and 1.50 nM, respectively). Ocular application of emedastine prior to histamine challenge inhibits vascular permeability in guinea pigs. Formulations containing emedastine have been used in the treatment of allergic conjunctivitis.
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分子式 |
C17H26N4O.2C4H4O4
|
分子量 |
534.6
|
CAS号 |
87233-62-3
|
中文名称 |
富马酸依美斯汀
|
储存方式 |
-20°C
|