The Lipophilic Properties of Angiotensin I-Converting Enzyme Inhibitors Do Not Influence Their Diffusion Through Cultured Endothelium

The Japanese Journal of Pharmacology

Benedikt Ball¹  Peter Dominiak¹  Andreas Dendorfer¹  Walter Raasch¹ 

[1]Institute of Experimental and Clinical Pharmacology and Toxicology, Medical University of Luebeck

关键词: Lipophilic property;    Angiotensin I-converting enzyme (ACE);    ACE inhibitor;    Membrane penetration;    Endothelium;   

DOI  :  10.1254/jjp.81.346

学科分类：药理学

来源: Nihon Yakuri Gakkai Henshuubu / Japanese Pharmacological Society

【 摘 要 】

References(21)Cited-By(6)The background for these investigations was the discovery that formation of angiotensin II by the renin angiotensin system can take place in extravascular tissues (e.g., cardiomyocytes and neurons) and within single cells. Consequently, the question arose about whether such tissue-based systems might be differentially influenced by angiotensin I-converting enzyme (ACE) inhibitors with distinct physicochemical properties. Therefore, the aim of this study was to investigate how the membrane penetration of various ACE inhibitors depends on their lipophilia. All diacid forms of ACE inhibitors are dissociated at a pH of 7.4 and scarcely extractable into octanol (extraction coefficient <10%). In contrast, the extraction coefficients of the parent substances showed marked differences in the following order of increasing lipophilia: enalapril=perindopril -->

【 授权许可】

Unknown