Bilastine

组胺H1受体拮抗剂(IC50=180nM)；100µM浓度下体外对30种受体中的组胺H1受体具有选择性；可预防豚鼠皮下注射组胺引起的微血管外渗(ED50=185µg/kg，静脉注射)、支气管痉挛(ED50=4.6µg/kg，静脉注射)和全身过敏反应(ED50=0.2µg/kg，口服)；可预防致敏大鼠皮下注射7.6和6.0mg/kg卵清蛋白或DNP引起的过敏反应。A histamine H1 receptor antagonist (IC50 = 180 nM); selective for the histamine H1 receptor in a panel of 30 receptors in vitro at 100 µM; 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; prevents anaphylaxis induced by subcutaneous administration of ovalbumin or DNP in sensitized rats at 7.6 and 6.0 mg/kg, respectively.