Captopril-d3 is intended for use as an internal standard for the quantification of captopril by GC- or LC-MS. Captopril is a first generation nonpeptidic ACE inhibitor (IC50 = 6.3 nM) that was designed based on bradykinin-potentiating peptides isolated from the venom of B. jararaca, a pit viper native to Brazil. 1,2,3 It does not exhibit a domain preference for binding either the C- or N-terminal active sites of the somatic form of ACE.1 Acute and chronic administration of captopril reduces blood pressure in spontaneously hypertensive Wistar-Kyoto rats and does not induce hypotension in salt-repleted normotensive Wistar-Kyoto rats.4 Captopril is also a competitive and reversible inhibitor of leukotriene (LTA4) hydrolase, which results in the disruption of LTB4 synthesis with an IC50 value of 14 μM.5
References
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2. Redelinghuys, P., Nchinda, A.T., and Sturrock, E.D. Development of domain-selective angiotensin I-converting enzyme inhibitors. Ann. N.Y. Acad. Sci 1056, 160-175 (2005).
3. Cushman, D.W., and Ondetti, M.A. Design of angiotensin converting enzyme inhibitors. Nat. Med. 5(10), 1110-1113 (1999).
4. Rubin, B., Antonaccio, M.J., and Horovitz, Z.P. Captopril (SQ 14,225) (D-3-mercapto-2-methylpropranoyl-L-proline): A novel orally active inhibitor of angiotensin-converting enzyme and antihypertensive agent. Prog. Cardiovasc. Dis. 21(3), 183-194 (1978).
5. Orning, L., Krivi, G., Bild, G., et al. Inhibition of leukotriene A4 hydrolase/aminopeptidase by captopril. J. Biol. Chem. 266(25), 16507-16511 (1991).