| 规格: | 98% |
| 分子量: | 422.5 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
Background:
Emedastine-13C-d3is intended for use as an internal standard for the quantification of emedastine by GC- or LC-MS. Emedastine is a histamine H1receptor antagonist (Ki= 1.3 nM).1It is selective for histamine H1over H2and H3receptors (Kis = 49 and 12.43 µM, respectively), as well as α1-, α2-, and β1-adrenergic and dopamine D1and D2receptors, and the serotonin (5-HT) receptor subtypes 5-HT1and 5-HT2at 10 µM.1,2Emedastine inhibits histamine-induced phosphoinositide turnover and intracellular calcium mobilization in primary human conjunctival epithelial cells (HCECs; IC50s = 1.6 and 2.9 nM, respectively).3It also inhibits histamine-stimulated secretion of IL-6, IL-8, and GM-CSF by primary HCECs (IC50s = 2.23, 3.42, and 1.50 nM, respectively).4Ocular application of emedastine prior to histamine challenge inhibits vascular permeability in guinea pigs.2Formulations containing emedastine have been used in the treatment of allergic conjunctivitis.
1.Sharif, N.A., Su, S.X., and Yanni, J.M.Emedastine: A potent, high affinity histamine H1-receptor-selective antagonist for ocular use: Receptor binding and second messenger studiesJ. Ocul. Pharmacol.10(4)653-664(1994) 2.Yanni, J.M., Stephens, D.J., Parnell, D.W., et al.Preclinical efficacy of emedastine, a potent, selective histamine H1 antagonist for topical ocular useJ. Ocul. Pharmacol.10(4)665-675(1994) 3.Sharif, N.A., Xu, S.X., Magnino, P.E., et al.Human conjunctival epithelial cells express histamine-1 receptors coupled to phosphoinositide turnover and intracellular calcium mobilization: Role in ocular allergic and inflammatory diseasesExp. Eye Res.63(2)169-178(1996) 4.Weimer, L.K., Gamache, D.A., and Yanni, J.M.Histamine-stimulated cytokine secretion from human conjunctival epithelial cells: Inhibition by the histamine H1 antagonist emedastineInt. Arch. Allergy. Immunol.115(4)288-293(1998)
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