Formulation: A solid
Formal Name: 1-(2-ethoxyethyl)-2-(hexahydro-4-methyl-13C-d3-1H-1,4-diazepin-1-yl)-1H-benzimidazole, 2E-butenedioate
Purity: ≥99% deuterated forms (d1-d3)
Formula Markup: C16[13C]H23D3N4O • C4H4O4
Formula Weight: 422,5
Shelf life (days): 1460
Notes: Emedastine-13C-d3 is intended for use as an internal standard for the quantification of emedastine (Item No. 23946) by GC- or LC-MS. Emedastine is a histamine H1 receptor antagonist (Ki = 1.3 nM).{38529} It is selective for histamine H1 over H2 and H3 receptors (Kis = 49 and 12.43 µM, respectively), as well as α1-, α2-, and β1-adrenergic and dopamine D1 and D2 receptors, and the serotonin (5-HT) receptor subtypes 5-HT1 and 5-HT2 at 10 µM.{38529,38530} Emedastine inhibits histamine-induced phosphoinositide turnover and intracellular calcium mobilization in primary human conjunctival epithelial cells (HCECs; IC50s = 1.6 and 2.9 nM, respectively).{38531} It 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).{38532} Ocular application of emedastine prior to histamine challenge inhibits vascular permeability in guinea pigs.{38530} Formulations containing emedastine have been used in the treatment of allergic conjunctivitis.
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