Ebastine

Ebastine is a histamine H₁ receptor antagonist and prodrug form of carebastine (Item No. 23076).¹ Ebastine binds to histamine H₁ receptors with an IC₅₀ value of 45 nM. It is selective for histamine H₁ receptors over α₁-adrenergic and muscarinic M₁ and M₂ receptors (IC₅₀s = 183, 1,100, and >10,000 nM, respectively), as well as dopamine D₂ receptors and the serotonin (5-HT) receptor subtype 5-HT_1A at 1 and 10 µM, respectively.² Ebastine (1, 5, and 10 µM) inhibits T cell proliferation and the production of IL-4 and IL-5 in isolated human T cells.³ It also reduces phytohemagglutinin-induced T cell migration and decreases LPS-induced IL-6 and TNF-α production by macrophages isolated from peripheral blood mononuclear cells (PBMCs). Ebastine inhibits histamine-induced and allergen-induced bronchospasm in guinea pigs (ED₅₀s = 115 and 334 µg/kg, respectively).⁴ Formulations containing ebastine have been used in the treatment of allergic rhinitis and chronic idiopathic urticaria.

WARNING This product is not for human or veterinary use.

1. Vincent, J., Liminana, R., Meredith, P.A., et al. The pharmacokinetics, antihistamine and concentration-effect relationship of ebastine in healthy subjects. Br. J. Clin. Pharmacol. 26(5), 497-502 (1988).

2. Abou-Gharbia, M., Moyer, J.A., Nielsen, S.T., et al. New antihistamines: Substituted piperazine and piperidine derivatives as novel H1-antagonists. J. Med. Chem. 38(20), 4026-4032 (1995).

3. Nori, M., Iwata, S., Munakata, Y., et al. Ebastine inhibits T cell migration, production of Th2-type cytokines and proinflammatory cytokines. Clin. Exp. Allergy 33(11), 1544-1554 (2003).

4. Llupià, J., Gras, J., and Llenas, J. Comparative antiallergic effects of second-generation H1-antihistamines ebastine, cetirizine and loratadine in preclinical models. Arzneimittelforschung 53(2), 93-97 (2003).