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Abstract
Moexipril is a long-acting, non-sulfhydryl angiotensine-converting enzyme inhibitor. It is used for treatment of arterial hypertension. Moexipril is the prodrug, yielding moexiprilat by hydrolysis of an ethyl ester group. Moexiprilat is the metabolite responsible for the pharmacological effect after moexipril administration. Samples of rat and human microsomai preparations exposed to moexipril treatment were analyzed by HPLC using octyl silica stationary phase and isocratic elution. To detect moexipril and moexiprilat the separation was monitored by both ultraviolet and mass specific detection. The rat liver microsomal preparation was more effective to in producing moexiprilat than the similar one derived from human liver cell lines. While additional potential metabolites of moexipril were suggested by computer-modeling, moexiprilat was the sole metabolite detected after microsomal treatment.
Keywords: Moexipril metabolism, moexiprilat, microsomal, HPLC-ES-MS, isocratic elution
Medicinal Chemistry
Title: Metabolism of Moexipril to Moexiprilat: Determination of In Vitro Metabolism Using HPLC-ES-MS
Volume: 3 Issue: 1
Author(s): H. Kalasz, G. Petroianu, K. Tekes, I. Klebovich, K. Ludanyi and Zs. Gulyas
Affiliation:
Keywords: Moexipril metabolism, moexiprilat, microsomal, HPLC-ES-MS, isocratic elution
Abstract: Moexipril is a long-acting, non-sulfhydryl angiotensine-converting enzyme inhibitor. It is used for treatment of arterial hypertension. Moexipril is the prodrug, yielding moexiprilat by hydrolysis of an ethyl ester group. Moexiprilat is the metabolite responsible for the pharmacological effect after moexipril administration. Samples of rat and human microsomai preparations exposed to moexipril treatment were analyzed by HPLC using octyl silica stationary phase and isocratic elution. To detect moexipril and moexiprilat the separation was monitored by both ultraviolet and mass specific detection. The rat liver microsomal preparation was more effective to in producing moexiprilat than the similar one derived from human liver cell lines. While additional potential metabolites of moexipril were suggested by computer-modeling, moexiprilat was the sole metabolite detected after microsomal treatment.
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Cite this article as:
Kalasz H., Petroianu G., Tekes K., Klebovich I., Ludanyi K. and Gulyas Zs., Metabolism of Moexipril to Moexiprilat: Determination of In Vitro Metabolism Using HPLC-ES-MS, Medicinal Chemistry 2007; 3 (1) . https://dx.doi.org/10.2174/157340607779317490
DOI https://dx.doi.org/10.2174/157340607779317490 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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