他齐茶碱
| 中文名称 | 他齐茶碱 |
|---|---|
| 中文同义词 | 他齐茶碱;(卤)-TAZIFYLLINE;(±)-TAZIFYLLINE;化合物 T10000 |
| 英文名称 | Tazifylline |
| 英文同义词 | Tazifylline;3,7-Dihydro-7-[2-hydroxy-3-[4-[3-(phenylthio)propyl]piperazin-1-yl]propyl]-1,3-dimethyl-1H-purine-2,6-dione;1H-Purine-2,6-dione, 3,7-dihydro-7-(2-hydroxy-3-(4-(3-(phenylthio)propyl)-1-piperazinyl)propyl)-1,3-dimethyl-;79712-53-1 (Dihydrochloride);Tazifilina;Tazifilina [spanish];Tazifylline [inn];Tazifyllinum |
| CAS号 | 79712-55-3 |
| 分子式 | C23H32N6O3S |
| 分子量 | 472.6 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 79712-55-3.mol |
| 结构式 |  |
他齐茶碱 性质
| 沸点 | 705.1±70.0 °C(Predicted) |
|---|---|
| 密度 | 1.34±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) | 14.27±0.20(Predicted) |
H1-receptor
Tazifylline potently inhibits contractions evoked by stimulation of histamine H1-receptors in isolated guinea pig ilea and exhibits high affinity for these receptors in radioligand binding studies in vitro Tazifylline has much lower affinity for histamine H2-receptors, alpha- and beta-adrenoceptors, 5-hydroxytryptamine and muscarinic receptor subtypes. Tazifylline poorly inhibits the release of histamine from rat peritoneal mast cells.
In rats, guinea pigs and dogs the antihistaminic effect of Tazifylline is rapid in onset and long-lived. In anesthetized guinea pigs, Tazifylline markedly inhibits histamine-induced bronchoconstriction and protects conscious animals from the lethal effect of large doses of the amine. In conscious rats, Tazifylline is more potent in reducing the inflammatory effects of intradermal histamine than that evoked by anaphylactic reaction. In conscious dogs, orally administered Tazifylline inhibits histamine-induced skin inflammation for long periods of time and in anesthetized animals attenuated that portion of the histamine-evoked hypotension attributable to stimulation of H1-receptors. Large oral doses of Tazifylline does not reduce spontaneous locomotor activity in mice, nor do they produce overt symptoms of behavioral depression in conscious rats.