113418-56-7
| 中文名称 | 113418-56-7 |
|---|---|
| 中文同义词 | 化合物 T13352;化合物WY 49051 |
| 英文名称 | 3,7-Dihydro-1,3-dimethyl-7-[3-[4-(diphenylmethoxy)-1-piperidinyl]propyl]-1H-purine-2,6-dione |
| 英文同义词 | 3,7-Dihydro-1,3-dimethyl-7-[3-[4-(diphenylmethoxy)-1-piperidinyl]propyl]-1H-purine-2,6-dione;Wy-49051;1H-Purine-2,6-dione, 7-[3-[4-(diphenylmethoxy)-1-piperidinyl]propyl]-3,7-dihydro-1,3-dimethyl- |
| CAS号 | 113418-56-7 |
| 分子式 | C28H33N5O3 |
| 分子量 | 487.59 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 113418-56-7.mol |
| 结构式 |  |
113418-56-7 性质
| 沸点 | 672.7±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.25±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 固体 |
| 酸度系数(pKa) | 8.32±0.10(Predicted) |
| 颜色 | 浅黄至黄色 |
Wy 49051 是一种有效的，可口服的 H1 receptor 拮抗剂，IC50 值为 44 nM。
IC50: 44 nM (H1 receptor)
Wy 49051 shows great inhibitory effect on H1, producing 92% inhibition of the histamine-induced contraction of the guinea pig ileum at a concentration 100 nM. Wy 49051 is the most potent compound with 700 times the potency of astemazole, 470 times the potency of chlorpheniramine. Wy 49051 also has high affinity for α1 receptor with IC 50 of 8 nM.
Wy 49051 shows potent activity against histamine-induced lethality in the guinea pig, with ED 50 of 1.91 mg/kg by po, 0.70 mg/kg by ip, and 0.01 mg/kg by iv. The duration of action of 24 is also favorable since there is no decrease in oral efficacy up to 18 h posttreatment.