Bilastine

Bilastine is a histamine H1 receptor antagonist (IC50 = 180 nM). 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. 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.Formal Name: 4-[2-[4-[1-(2-ethoxyethyl)-1H-benzimidazol-2-yl]-1-piperidinyl]ethyl]-alpha,alpha-dimethyl-benzeneacetic acid. CAS Number: 202189-78-4. Synonyms: F-96221-BM1. Molecular Formula: C28H37N3O3. Formula Weight: 463.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: Chloroform: 30 mg/ml. SMILES: CCOCCN1C(C2CCN(CCC3=CC=C(C(C)(C)C(O)=O)C=C3)CC2)=NC4=CC=CC=C41. InChi Code: InChI=1S/C28H37N3O3/c1-4-34-20-19-31-25-8-6-5-7-24(25)29-26(31)22-14-17-30(18-15-22)16-13-21-9-11-23(12-10-21)28(2,3)27(32)33/h5-12,22H,4,13-20H2,1-3H3,(H,32,33). InChi Key: ACCMWZWAEFYUGZ-UHFFFAOYSA-N.