215529-47-8

中文名称 215529-47-8

英文名称 Bamirastine

CAS 215529-47-8

分子式 C31H37N5O3

分子量 527.66

MOL 文件 215529-47-8.mol

215529-47-8 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

巴麦斯汀

英文别名

TAK-427
Bamirastine
Imidazo[1,2-b]pyridazine-2-acetic acid, 6-[[3-[4-(diphenylmethoxy)-1-piperidinyl]propyl]amino]-α,α-dimethyl-

物理化学性质

熔点109-112 °C

密度1.23±0.1 g/cm3(Predicted)

储存条件-20°C储存

溶解度溶于二甲基亚砜

酸度系数(pKa)2.29±0.10(Predicted)

常见问题列表

生物活性

Bamirastine 抑制配体结合到重组人组胺 H1 受体 (rhH1R)，IC50 为 17.3 nM。

靶点

IC50: 17.3 nM (rhH ₁ R)

体外研究

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.

体内研究

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.