Bepotastine-d₆ (besylate)

Bepotastine-d₆ is intended for use as an internal standard for the quantification of bepotastine (Item No. 23721) by GC- or LC-MS. Bepotastine is an antagonist of the histamine H₁ receptor that is selective over H₃, α₁-, α₂-, and β-adrenergic, dopamine D_2long, serotonin 5-HT₂, muscarinic acetylcholine, and benzodiazepine receptors.¹ It reduces dye leakage from the nasal passages of rats acutely sensitized to an antigen (ED₅₀ = 0.03 mg/kg) and inhibits histamine-induced bronchoconstriction in the anesthetized dog (ED₅₀ = 3.2 µg/kg).^2,3 Bepotastine prevents conjunctival vascular hyperpermeability in a guinea pig model of conjunctivitis in a dose-dependent manner.⁴ Formulations containing bepotastine have been used in the treatment of itching associated with allergic conjunctivitis.

WARNING This product is not for human or veterinary use.

1. Kato, M., Nishida, A., Aga, Y., et al. Pharmacokinetic and pharmacodynamic evaluation of central effect of the novel antiallergic agent betotastine besilate. Arzneimittelforschung. 47(10), 1116-1124 (1997).

2. Murata, T., Matsumoto, Y., Suzuki, T., et al. Effect of betotastine besilate (TAU-284), a novel anti-allergic agent, on experimental allergic rhinitis. Arerugi 46(7), 576-584 (1997).

3. Matsubara, S., Ono, C., Yamazaki, N., et al. Inhibitory effects of bepotastine, a novel anti-allergic drug on histamine-induced bronchoconstriction in anesthetized dogs. Yakuri to Chiryo 25(4), 895-900 (1997).

4. Kida, T., Fuji, A., Sakai, O., et al. Bepotastine besilate, a highly selective histamine H₁ receptor antagonist, suppresses vascular hyperpermeability and eosinophil recruitment in in vitro and in vivo experimental allergic conjunctivitis models. Exp. Eye Res. 91(1), 85-91 (2010).