产品描述:
Bilastine is a histamine H1 receptor antagonist (IC50 = 180 nM).{42911} It is selective for the histamine H1 receptor in a panel of 30 receptors in vitro at 100 µM. Bilastine prevents microvascular extravasation (ED50 = 185 µg/kg, i.v.), bronchospasm (ED50 = 4.6 µg/kg, i.v.), and systemic anaphylaxis (ED50 = 0.2 µg/kg, p.o.) induced by subcutaneous histamine in guinea pigs.{42912} It prevents anaphylaxis induced by subcutaneous administration of ovalbumin or dinitrophenylated human albumin (DNP) in sensitized rats when administered at doses of 7.6 and 6.0 mg/kg, respectively. Formulations containing bilastine have been used in the treatment of urticaria and allergic rhinitis.