Ro-15-2041
| 中文名称 | Ro-15-2041 |
|---|---|
| 中文同义词 | 化合物 T12741 |
| 英文名称 | Ro-15-2041 |
| 英文同义词 | Imidazo[2,1-b]quinazolin-2(3H)-one, 7-bromo-1,5-dihydro-3,6-dimethyl-;Ro152041,Ro 15 2041 |
| CAS号 | 77448-87-4 |
| 分子式 | C12H12BrN3O |
| 分子量 | 294.15 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 77448-87-4.mol |
| 结构式 |  |
Ro-15-2041 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | 溶于二甲基亚砜 |
phosphodiesterase
Ro 15-2041 inhibits platelet aggregation induced by all common platelet agonists in platelet-rich plasma obtained from various species including man (IC 50 =1-3 μM). Ro 15-2041 potentiates platelet inhibition by prostacyclin, the prostacyclin-induced increase of intraplatelet cyclic (c) AMP levels and inhibits the collagen-induced release of serotonin and beta-thromboglobulin. Ro 15-2041 reduces the increase and accelerated the normalization of cytosolic free Ca 2+ in thrombin-stimulated human platelets. Ro 15-2041 is a potent (IC 50 =70 nM) and selective inhibitor of platelet cAMP-phosphodiesterase activity. Whereas Ro 15-2041 causes complete inhibition of cAMP-phosphodiesterase activity in human platelet supernatants, breakdown of cAMP in cardiac homogenates is depressed to maximally 50%. In human brain and rabbit uterus Ro 15-2041 is at least 1000 times less potent. By comparison, papaverine fully inhibits phosphodiesterase activity in all four tissues with similar IC 50 values of about 5 μM. Furthermore, Ro 15-2041 selectively inhibits cAMP-phosphodiesterase activity of a bovine calmodulin-independent but not of a calmodulin-dependent enzyme preparation.