108427-72-1
基本信息
4H-Pyrido[1,2-a]pyrimidin-4-one, 9-[(4-acetyl-3-hydroxy-2-propylphenoxy)methyl]-3-(2H-tetrazol-5-yl)-
3-(1H-Tetrazol-5-yl)-9-[[[2-propyl-3-hydroxy-4-(methylcarbonyl)phenyl]oxy]methyl]-4H-pyrido[1,2-a]pyrimidin-4-one
物理化学性质
| 熔点 | 269-271 °C |
| 沸点 | 678.8±65.0 °C(Predicted) |
| 密度 | 1.46±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) | 3?+-.0.10(Predicted) |
常见问题列表
|
LTE 4 3 nM (IC 50 , In isolated guinea pig ileum) |
LTD 4 4 nM (IC 50 , In isolated guinea pig ileum) |
LTC 4 8 nM (IC 50 , In isolated guinea pig ileum) |
In isolated guinea pig preparations, AS-35 antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC 50 values of 8 nM, 4 nM and 3 nM, respectively. In the trachea, the agent also antagonizes LTD4 and LTE4-induced con tractions with IC 50 values of 10 nM and 20 nM, respectively. However, AS-35 does not antagonize LTC4-induced tracheal contraction in the presence of L-serine borate.
AS-35 (0.0375 to 0.3 mg/kg, i.v.) dose-dependently antagonizes bronchoconstriction induced by i.v.-injection of LTC4 and LTD4 in anesthetized guinea pigs, but does not inhibit histamine-induced bronchoconstriction. Oral administration of AS-35 also antagonizes LTD4 as well as antigen-induced LT-mediated bronchoconstriction. AS-35 (p.o.) inhibits LTD4-induced increase in the cutaneous vascular permeability of guinea pig.