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215529-47-8

中文名稱 215529-47-8
英文名稱 Bamirastine
CAS 215529-47-8
分子式 C31H37N5O3
分子量 527.67
MOL 文件 215529-47-8.mol
215529-47-8 結(jié)構(gòu)式 215529-47-8 結(jié)構(gòu)式

基本信息

中文別名
巴麥斯汀
英文別名
TAK-427
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)

熔點109-112 °C
密度1.23±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)2.29±0.10(Predicted)

常見問題列表

生物活性
Bamirastine 抑制配體結(jié)合到重組人組胺 H1 受體 (rhH1R),IC50 為 17.3 nM。
靶點

IC50: 17.3 nM (rhH 1 R)

體外研究

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.

體內(nèi)研究

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.

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