The Effects of Captopril on Rat Aortic Angiotensin‐Converting Enzyme
The Effects of Captopril on Rat Aortic Angiotensin‐Converting Enzyme
复制标题
卡托普利对大鼠主动脉血管紧张素转换酶的影响
DOI：
10.1097/00005344-198203000-00022
复制
发表时间：
1982
影响因子：
3
通讯作者：
B. L. Bean
中科院分区：
文献类型：
--
作者：
P. Velletri;B. L. Bean
使用放射酶技术发现大鼠主动脉内存在血管紧张素转换酶（ACE）活性。42%的酶活性位于图尼卡中膜内。使用平衡透析池系统，确保血浆和主动脉中的游离卡托普利浓度相等，观察到两种组织中的转化酶具有相似的抑制剂解离常数。四个每日腹腔内剂量，但不是一个单一的剂量，卡托普利导致了持续的抑制后24小时，最后一次给药的前列腺素转化酶。此时血浆转化酶活性未发生变化。这些结果表明，不同的转化酶库以不同的速率从卡托普利抑制中恢复。主动脉ACE的长期抑制血管壁内的药物积累方面进行了讨论，并讨论了这种积累对持续的抗高血压作用的巯甲丙脯酸的影响。
Summary Angiotensin-converting enzyme (ACE) activity was found to be present within the rat aorta using radioenzymatic techniques. Forty-two percent of the enzyme activity was localized within the tunica media. Using an equilibrium dialysis cell system that insured equal free captopril concentrations in both plasma and aorta, converting enzyme in both tissues was observed to possess similar dissociation constants for the inhibitor. Four daily intraperitoneal doses, but not a single dose, of captopril led to a persistent inhibition of aortic-converting enzyme 24 h after the final drug administration. Plasma-converting enzyme activity was unchanged at this time. These results suggest that different pools of converting enzyme recover from captopril inhibition at different rates. The prolonged inhibition of aortic ACE is discussed in terms of drug accumulation within the vessel wall, and the effects of such accumulation on the persistent antihypertensive actions of captopril are also discussed.