An internal standard for the quantification of epinastine
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Unlabeled Version(s)
18136Epinastine (hydrochloride)
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Epinastine-13C-d3 (hydrobromide)

Item No. 30089

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepin-1-13C-1,1,13b-d3-3-amine, monohydrobromide
Synonyms
  • WAL 801CL-13C-d3
Molecular Formula
C15[13C]H12D3N3 • HBr
Formula Weight
334.2
Purity
≥99% deuterated forms (d1-d3)
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: solubleWater: soluble
SMILES
NC1=N[13C]([2H])([2H])C2([2H])C(C=CC=C3)=C3CC(C=CC=C4)=C4N21.Br
InChi Code
InChI=1S/C16H15N3.BrH/c17-16-18-10-15-13-7-3-1-5-11(13)9-12-6-2-4-8-14(12)19(15)16;/h1-8,15H,9-10H2,(H2,17,18);1H/i10+1D2,15D;
InChi Key
ADPMHRDERZTFIN-CRIIMPNVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $480

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    Product Description

    Epinastine-13C-d3 is intended for use as an internal standard for the quantification of epinastine (Item No. 18136) by GC- or LC-MS. Epinastine is a histamine H1 receptor antagonist (apparent Kis = 1.41 and 1.62 nM using guinea pig cerebellar and lung membranes, respectively) and mast cell stabilizer.1,2 It inhibits IgE-induced histamine, TNF-α, and IL-10 secretion in human cord blood stem cell-derived mast cells (CBMCs) when used at a concentration of 0.1 μg/ml.2 Epinastine inhibits histamine-induced cutaneous vascular permeability in rats and bronchoconstriction in anesthetized guinea pigs (ID50s = 5 and 0.1 mg/kg, respectively).3 It inhibits dye leakage into the conjunctiva in a rat model of passive anaphylaxis reaction-induced vascular hyperpermeability of the conjunctiva (ID50 = 9.7 mg/kg, p.o.).4 Topical administration of formulations containing epinastine (0.05% three times per day) reduces lid edema, tearing, and redness, as well as the number of neutrophils and eosinophils in the lid fornix, in a mouse model of atopic conjunctivitis.2 Formulations containing epinastine have been used in the prevention of itching associated with allergic conjunctivitis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ter Laak, A.M., Donné-Op den Kelder, G.M., Bast, A., et al. Is there a difference in the affinity of histamine H1 receptor antagonists for CNS and peripheral receptors? An in vitro study. Eur. J. Pharmacol. 232(2-3), 199-205 (1993).

    2. Galatowicz, G., Ajayi, Y., Stern, M.E., et al. Ocular anti-allergic compounds selectively inhibit human mast cell cytokines in vitro and conjunctival cell infiltration in vivo. Clin. Exp. Allergy 37(11), 1648-1656 (2007).

    3. Matsushita, K., Nobutoshi, A., and Aritake, K. Pharmacological studies on the novel antiallergic drug HQL-79: II. Elucidation of mechanisms for antiallergic and antiasthmatic effects. Jpn. J. Pharmacol. 78(1), 11-22 (1998).

    4. Tamura, T., Sato, H., Miki, I., et al. Effects of orally administered olopatadine hydrochloride on the ocular allergic reaction in rats. Allergol. Int. 52(2), 77-83 (2003).