129981-36-8
129981-36-8 結(jié)構(gòu)式
基本信息
中文別名
山帕曲拉 英文別名
UK-81252sampatrilat
L-Tyrosine, N2-(methylsulfonyl)-L-lysyl-1-[(2S)-3-amino-2-carboxypropyl]cyclopentanecarbonyl-
常見問題列表
生物活性
Sampatrilat (UK-81252) 是一種強效具有口服活性的血管肽酶抑制劑，可抑制血管緊張素轉(zhuǎn)換酶 (ACE) 和中性血管內(nèi)肽酶 (NEP)。Sampatrilat 對 C-domain ACE (Ki=13.8 nM) 的抑制作用是 N-domain 的 12.4 倍 (Ki=171.9 nM)。Sampatrilat (UK-81252) 可用于慢性心力衰竭和血壓調(diào)節(jié)的相關(guān)研究。靶點
Ki: 13.8 nM (cACE); 171.9 nM (nACE)
體內(nèi)研究
Sampatrilat (oral adminstration; 30 mg/kg; once a day; 5 weeks) reduces the mortality of the rats with CAL (20% versus 57% for untreated rats) and increase in the survival rate and improvement of hemodynamic function of the rats with CAL. This compound suppresses tissue ACE and neutral endopeptidase (NEP) activities, but it does not affect the arterial blood pressure, whereas it attenuates the CAL-induced increases in the left ventricular end-diastolic pressure, heart weight, and collagen content of the viable left Ventricle.
| Animal Model: | Left coronary artery ligation (CAL) and sham-operated rats |
| Dosage: | 30 mg/kg |
| Administration: | Oral adminstration |
| Result: | Prevented the increases in heart weight and cardiac collagen content of the rats with CAL. |