215529-47-8
| 中文名称 | 215529-47-8 |
|---|---|
| 中文同义词 | 巴麦斯汀;化合物 T13566 |
| 英文名称 | Bamirastine |
| 英文同义词 | Bamirastine;TAK-427;Imidazo[1,2-b]pyridazine-2-acetic acid, 6-[[3-[4-(diphenylmethoxy)-1-piperidinyl]propyl]amino]-α,α-dimethyl- |
| CAS号 | 215529-47-8 |
| 分子式 | C31H37N5O3 |
| 分子量 | 527.67 |
| EINECS号 | |
| 相关类别 | 制剂-抑制剂 |
| Mol文件 | 215529-47-8.mol |
| 结构式 |  |
215529-47-8 性质
| 熔点 | 109-112 °C |
|---|---|
| 密度 | 1.23±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 2.29±0.10(Predicted) |
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.