Perindopril erbumine 是一种长效血管紧张素转换酶抑制剂。

Perindopril Erbumine is the tert-butylamine salt of perindopril, the ethyl ester of a non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Upon hydrolysis, perindopril erbumine is converted to its active form perindoprilat, inhibiting ACE and the conversion of angiotensin I to angiotensin II; consequently, angiotensin II-mediated vasoconstriction and angiotensin II-stimulated aldosterone secretion from the adrenal cortex are inhibited and diuresis and natriuresis ensue.

在阿尔兹海默症大鼠体内,Perindopril Erbumine（1 mg/kg/day）可使海马ACE活性明显受到抑制,并预防脑损伤和认知障碍.Perindopril Erbumine（3 mg/kg/day）抑制6.4% 的体内RAECs细胞凋亡（脂多糖诱导）,而ramipril的抑制率只有3.2%.Perindopril Erbumine（2 mg/kg/day,p.o. ）可使SCC-VII肿瘤生长被显著抑制,并通过对VEGF诱导血管生成的抑制作用,减少肿瘤周围血管形成.Perindopril Erbumine（2 mg/kg/day,p.o. ）可强烈抑制大鼠体内BNL-HCC肿瘤生长,这效果与每天口服20 mg/kg类似,但每天口服20 mg/kgAT1-R拮抗剂losartan或candesartan则无抑制作用.

Perindopril Erbumine抑制突变血管紧张素转换酶（包含两个活性区域）的血管紧张素-和Aβ42-到-Aβ40的转化活性,IC50分别为0.03-0.1 μM和0.01-0.03 μM。Perindopril Erbumine（2 μM）对KB和SCC-VII细胞无明显细胞毒性,但能浓度依赖性地使KB细胞中血管紧张素II的产生和VEGF的转录显著减少。与血管紧张素转化酶的血管紧张素I结合位点相比,Perindopril Erbumine对缓激肽结合位点的结合亲和力更高,缓激肽/血管紧张素I选择性比率为1.44。

107133-36-8

C23H43N3O5

441.613

S9490-3;培哚普利叔丁胺盐;Perindopril tert-butylamine salt;培哚普利叔丁胺

H2O:50 mg/mL (113.22 mM)
DMSO:10 mg/mL (22.64 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years