Bilastine is a second-generation antihistamine used for allergic rhinoconjunctivitis and urticaria (hives). Bilastine also has anti-inflammatory activity.
|Mechanism of Action||Bilastine, a novel molecule, is a selective histamine H1 receptor antagonist. It is a substrate for P-glycoprotein, a membrane pump|
|Eukaryotic Cell Culture Applications||Bilastine binds to histamine H1-receptors as indicated by its displacement of [3H]-pyrilamine from H1-receptors expressed in guinea-pig cerebellum and human embryonic kidney (HEK) cell lines. Bilastine is selective for histamine H1-receptors as shown in receptor-binding screening with 30 different receptors. The specificity of its H1-receptor antagonistic activity was also demonstrated in a series of in vitro experiments with guinea-pig and rat tissues. Bilastine also has anti-inflammatory activity as demonstrated in vitro with the Schultz-Dale reaction (Corcóstegui et al, 2005).|
|References||Church MK and Labeaga L (2017) Bilastine: a new H1-antihistamine with an optimal profile for updosing in urticaria. J. Eur. Acad. Dermatol, Venereol 31(9):1447-1452 PMID 28467671 Corcóstegui R, Labeaga L, Innerárity A, Berisa A, Orjales A (2005) Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: Receptor selectivity and in vitro antihistaminic activity. Drugs R D.6(6):371-84 PMID 16274260|