匹伏普利
| 中文名称 | 匹伏普利 |
|---|---|
| 中文同义词 | 匹伏普利;化合物 T16544 |
| 英文名称 | Pivopril |
| 英文同义词 | Pivopril;N-Cyclopentyl-N-[(S)-3-[(2,2-dimethyl-1-oxopropyl)thio]-2-methyl-1-oxopropyl]glycine;RHC 3659(S);Glycine, N-cyclopentyl-N-[(2S)-3-[(2,2-dimethyl-1-oxopropyl)thio]-2-methyl-1-oxopropyl]- |
| CAS号 | 81045-50-3 |
| 分子式 | C16H27NO4S |
| 分子量 | 329.45 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 81045-50-3.mol |
| 结构式 |  |
匹伏普利 性质
| 沸点 | 490.4±38.0 °C(Predicted) |
|---|---|
| 密度 | 1.16±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) | 3.49±0.10(Predicted) |
ACE
Pivalopril is a new compound with a hindered sulfur group that has been compared to Captopril for oral angiotensin-converting enzyme (ACE) inhibition in rats and dogs and antihypertensive activity in rats. In separate groups of conscious normotensive rats, Pivalopril (0.03-1.0 mg/kg, orally [p.o.]) produces a dose-related antagonism of angiotensin I (AngI)-induced pressor effects. The ED 50 for Pivalopril and Captopril is 0.1 mg/kg. In conscious normotensive dogs, Pivalopril (incremental doses of 0.01-1.0 mg/kg, p.o.) produces a dose-related antagonism of AngI pressor effects. The ED 50 is 0.17 mg/kg for Pivalopril and 0.06 mg/kg for Captopril. At equieffective doses the two compounds have similar durations of action. In sodium-deficient, conscious spontaneously hypertensive rats (SHR), Pivalopril (1-100 mg/kg, p.o.) produces a dose-related reduction in mean arterial pressure. The potency and duration are similar to those of Captopril. In the sodium-replete SHR, 5 days of oral dosing with Pivalopril (100 mg/kg per day) decreases mean arterial pressure more effectively than Captopril (100 mg/kg per day). It is concluded that Pivalopril is a potent, orally effective ACE inhibitor and antihypertensive agent.