215529-47-8
215529-47-8 結(jié)構(gòu)式
基本信息
Bamirastine
Imidazo[1,2-b]pyridazine-2-acetic acid, 6-[[3-[4-(diphenylmethoxy)-1-piperidinyl]propyl]amino]-α,α-dimethyl-
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
IC50: 17.3 nM (rhH 1 R)
Bamirastine (TAK-427) reduces specific binding of [ 3 H] pyrilamine to recombinant human H 1 receptors (rhH 1 R) is seen in a concentration- dependent manner with an IC 50 value of 17.3 nM. The K i value is calculated to be 7.35 nM. The affinity of Bamirastine is found to be as high as that of azelastine, 2 times lower than that of Epinastine, 8 times lower than that of ketotifen and 3 times higher than that of Terfenadine.
Bamirastine (TAK-427) inhibits histamine induced skin reactions in guinea pigs and mice with an ID 50 value of 0.884 and 0.450 mg/kg, p.o., respectively; significant inhibition associated with 10 mg/kg of Bamirastine is still observed 24 h after dosing in guinea pigs. Even at 300 mg/kg, Bamirastine does not affect pentobarbital-induced sleeping time in mice. Bamirastine significantly inhibits passive cutaneous anaphylaxis (PCA) in mice and guinea pigs, and also inhibits antigen-induced ISRs in guinea pigs.