| Description | Libenzapril (CGS 16617) is a potent angiotensin-converting enzyme inhibitor used to study myocardial injury. |
| In vivo | The effect of intravenous (i.v.) libenzapril was studied in six healthy males by administering i.v. angiotensin I (AI) was administered in stepwise increments of 20 ng/kg/5 min until the subjects' systolic blood pressure (SBP) had increased 20-30 mm Hg above baseline. The mean baseline infusion of 63 ng/kg/5 min resulted in a significant (P < 0.05) increase in the ratio of AII to AI plasma levels from 0.52 +/- 0.46 to 7.92 +/- 4.48 and a SBP increase of 120 +/- 7.1 to 147 +/- 5.6. Within 15 minutes of starting the 1-mg infusion of libenzapril over 1.5 hours, the AII/AI ratio decreased to baseline values, and the SBP returned to baseline in 1 hour. Repeat AI challenges at 3.5 and 5 hours postdose did not increase SBP significantly. Even the 6.5-hour challenge demonstrated only a slight increase in SBP, with an AII/AI ratio of 0.26. At 24 hours, SBP was only 40% of the baseline response, demonstrating that libenzapril is a potent long-acting ACE inhibitor.[1] |
| Synonyms | CGS 16617, Abutapril |
| molecular weight | 363.41 |
| Molecular formula | C18H25N3O5 |
| CAS | 109214-55-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: < 1mg/ml (insoluble） |
| References | 1. Tang JP, Rakhit A, Douglas FL, Melethil S. Effect of chronic hypertension on the blood-brain barrier permeability of libenzapril. Pharm Res. 1992 Feb;9(2):236-43. PubMed PMID: 1553348. 2. Morgan JM, Piraino AJ, Saris SD, Graham CS, Hirschhorn WL, Kochak GM, Choi RL. Inhibition of angiotensin-converting enzyme with libenzapril in normotensive males. J Clin Pharmacol. 1994 Dec;34(12):1177-82. PubMed PMID: 7738213. 3. Kochak GM, Choi RL, deSilva JK, Reydel-Bax P. Pharmacodynamic dependent disposition of the angiotensin converting enzyme inhibitor, libenzapril. J Clin Pharmacol. 1990 Feb;30(2):138-43. PubMed PMID: 2312764. 4. Tang JP, Xu ZQ, Douglas FL, Rakhit A, Melethil S. Increased blood-brain barrier permeability of amino acids in chronic hypertension. Life Sci. 1993;53(25):PL417-20. PubMed PMID: 7902950. |