Bepotastine is a selective and orally active second-generation histamine H1 receptor antagonist. Bepotastine has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research.
IC50&Target
Histamine H1 receptor
体外研究
Bepotastine possesses additional anti-allergic activity including stabilization of mast cell function, inhibition of eosinophilic infiltration, inhibition of IL-5 production, and inhibition of leukotriene B4 (LTB4) and LTD4 activity.
Bepotastine significantly inhibits antigen-induced stimulation of IL-5 production in human peripheral blood mononuclear cells (PBMCs) at concentrations of 10-100 μM and the effect is enhanced when the PBMCs are pre-incubated with Bepotastine.
Leukotriene B4 increased Ca2+ concentration in cultured neutrophils, which is suppressed by Bepotastine besilate (1-100 μM). Leukotriene B4 increased Ca2+ concentration in cultured dorsal root ganglion neurons, which is also suppressed by Bepotastine besilate (100 μM).
体内研究
Bepotastine besilate (10 mg/kg) inhibits scratching induced by an intradermal injection of histamine (100 nmol/site), but not serotonin (100 nmol/site).
Bepotastine besilate (1-10 mg/kg, oral) dose-dependently suppresses scratching induced by substance P (100 nmol/site) and leukotriene B4 (0.03 nmol/site).
Bepotastine in vivo dose-dependently inhibits the acceleration of histamine-induced vascular permeability and inhibits homologous passive cutaneous anaphylaxis in guinea pig studies.
In mouse models of itching, oral Bepotastine inhibits the frequency and duration of scratching behavior.
分子式
C21H25N2O3Cl
分子量
388.89
CAS号
125602-71-3
中文名称
贝托司汀;贝他斯汀;贝托斯汀;贝他司汀
运输条件
Room temperature in continental US; may vary elsewhere.