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Captopril is an angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and some types of congestive heart failure.
Captopril was discovered in 1977.It was the first ACE inhibitor developed and was considered a breakthrough both because of its novel mechanism of action and also because of the revolutionary development process.Captopril was discovered and developed at E. R. Squibb & Sons Pharmaceuticals based on concepts pioneered by Nobel Laureate John Vane and is now marketed by Bristol-Myers Squibb.
Drosophila ACE in complex with captopril (purple), PDB entry 2x8z
Captopril's main uses are based on its vasodilation and inhibition of some renal function activities. These benefits are most clearly seen in: 1) Hypertension 2) Cardiac conditions such as congestive heart failure and after myocardial infarction 3) Preservation of kidney function in diabetic nephropathy
Additionally, it has shown mood-elevating properties in some patients. This is consistent with the observation that animal screening models indicate putative antidepressant activity for this compound, although one study has been negative. Formal clinical trials in depressed patients have not been reported.
It has also been investigated for use in the treatment of cancer.Captopril stereoisomers were also reported to inhibit some metallo-β-lactamases.
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