| 货号 | 18136-10mg |
| 描述 | Epinastine is a non-sedating ophthalmic antihistamine that antagonizes histamine H1 receptors (IC50 = 1.58 nM in guinea pigs) and prevents the release of pro-inflammatory mediators from mast cells and eosinophils.1,2 Although it can pass through the blood-brain barrier, the low brain distribution of epinastine is accounted for by efficient efflux transport by P-glycoproteins and poor uptake by the influx transporter.3 Epinastine also inhibits superoxide generation by rat neutrophils.4 |
| 别名 | WAL 801CL; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.ter Laak, A.M.,Venhorst, J.,Donné-Op den Kelder, G.M., et al. The histamine H1-receptor antagonist binding site. A stereoselective pharmacophoric model based upon (semi-)rigid H1-antagonists and including a known interaction site on the receptor. Journal of Medicinal Chemistry 38, 3351-3360 (1995). 2.Mochizuki, Y.I.,Furuta, A.,Furuya, A., et al. Suppressive activity of epinastine hydrochloride on eosinophil activation in vitro. In Vivo 22, 13-20 (2008). 3.Ishiguro, N.,Nozawa, T.,Tsujihata, A., et al. Influx and efflux transport of H1-antagonist epinastine across the blood-brain barrier. Drug Metabolism and Disposition 32(5), 519-524 (2004). 4.Fukuishi, N.,Kan, T.,Hirose, K., et al. Inhibitory effect of epinastine on superoxide generation by rat neutrophils. Japanese Journal of Pharmacology 68, 449-452 (1995). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 285.8 |
| 分子式 | C16H15N3 • HCl |
| CAS号 | 108929-04-0 |
| 稳定性 | ≥ 2 years |
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