Formulation: A crystalline solid
Formal Name: 4-[2-[4-[1-(2-ethoxyethyl)-1H-benzimidazol-2-yl]-1-piperidinyl]ethyl]-α,α-dimethyl-benzeneacetic acid
Purity: ≥98%
Formula Markup: C28H37N3O3
Formula Weight: 463,6
Shelf life (days): 1460
CAS Number: 202189-78-4
Notes: 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.
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