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Chemical Compound Review

Omapatrilat     (3S,7S,11S)-2-oxo-3-[[(2S)-3- phenyl-2...

Synonyms: AC1LCVB7, CHEMBL289556, CHEBI:159756, BMS-186716, CID656629, ...
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Disease relevance of D01970


High impact information on D01970


Chemical compound and disease context of D01970


Biological context of D01970


Anatomical context of D01970


Associations of D01970 with other chemical compounds

  • Dahl salt-sensitive rats (n = 6 per group) on standard or salt-enriched chow were treated for 8 wk with O (36 +/- 4 mg/kg per d), C (94 +/- 2 mg/kg per d), or placebo [2].
  • ENA and OMA administered beginning on day 2 after surgery were equally effective in normalizing systolic BP (SBP) and preventing glomerulosclerosis (GS) for 12 wk [4].
  • METHODS AND RESULTS: In a double-blind, placebo-controlled crossover study, single oral doses of the dual neutral endopeptidase-angiotensin-converting enzyme inhibitor, 10 mg BMS-186716 and the angiotensin-converting enzyme inhibitor fosinopril (20 mg) were administered to 9 normotensive subjects with induced mild sodium depletion [22].
  • Since RPF was not significantly affected, reduction of the filtration fraction was more marked in enalapril- than omapatrilat-treated rats (60 and 28%, respectively) [23].
  • Insulin increased cell proliferation, and addition of lisinopril, omapatrilat or irbesartan inhibited this effect [24].

Gene context of D01970


Analytical, diagnostic and therapeutic context of D01970


  1. Vasopeptidase inhibitors. Weber, M.A. Lancet (2001) [Pubmed]
  2. Vasopeptidase inhibition restores renovascular endothelial dysfunction in salt-induced hypertension. Quaschning, T., D'Uscio, L.V., Shaw, S., Gröne, H.J., Ruschitzka, F., Lüscher, T.F. J. Am. Soc. Nephrol. (2001) [Pubmed]
  3. Comparison of the effects of an angiotensin-converting enzyme inhibitor and a vasopeptidase inhibitor after myocardial infarction in the rat. Lapointe, N., Blais, C., Adam, A., Parker, T., Sirois, M.G., Gosselin, H., Clément, R., Rouleau, J.L. J. Am. Coll. Cardiol. (2002) [Pubmed]
  4. Vasopeptidase inhibition affords greater renoprotection than angiotensin-converting enzyme inhibition alone. Taal, M.W., Nenov, V.D., Wong, W., Satyal, S.R., Sakharova, O., Choi, J.H., Troy, J.L., Brenner, B.M. J. Am. Soc. Nephrol. (2001) [Pubmed]
  5. Comparison of the effects of omapatrilat and irbesartan/hydrochlorothiazide on endothelial function and cardiac hypertrophy in the stroke-prone spontaneously hypertensive rat: sex differences. Graham, D., Hamilton, C., Beattie, E., Spiers, A., Dominiczak, A.F. J. Hypertens. (2004) [Pubmed]
  6. Comparison of vasopeptidase inhibitor, omapatrilat, and lisinopril on exercise tolerance and morbidity in patients with heart failure: IMPRESS randomised trial. Rouleau, J.L., Pfeffer, M.A., Stewart, D.J., Isaac, D., Sestier, F., Kerut, E.K., Porter, C.B., Proulx, G., Qian, C., Block, A.J. Lancet (2000) [Pubmed]
  7. Renoprotective effects of vasopeptidase inhibition in an experimental model of diabetic nephropathy. Davis, B.J., Johnston, C.I., Burrell, L.M., Burns, W.C., Kubota, E., Cao, Z., Cooper, M.E., Allen, T.J. Diabetologia (2003) [Pubmed]
  8. Vasopeptidase inhibition with omapatrilat in chronic heart failure: acute and long-term hemodynamic and neurohumoral effects. McClean, D.R., Ikram, H., Mehta, S., Heywood, J.T., Rousseau, M.F., Niederman, A.L., Sequeira, R.F., Fleck, E., Singh, S.N., Coutu, B., Hanrath, P., Komajda, M., Bryson, C.C., Qian, C., Hanyok, J.J. J. Am. Coll. Cardiol. (2002) [Pubmed]
  9. Physiologic consequences of vasopeptidase inhibition in humans: effect of sodium intake. Azizi, M., Lamarre-Cliche, M., Labatide-Alanore, A., Bissery, A., Guyene, T.T., Ménard, J. J. Am. Soc. Nephrol. (2002) [Pubmed]
  10. Vasopeptidase inhibition and Ang-(1-7) in the spontaneously hypertensive rat. Ferrario, C.M., Averill, D.B., Brosnihan, K.B., Chappell, M.C., Iskandar, S.S., Dean, R.H., Diz, D.I. Kidney Int. (2002) [Pubmed]
  11. Comparison of the cardiovascular protection by omapatrilat and lisinopril treatments in DOCA-salt hypertension. Millette, E., Demeilliers, B., Wu, R., Laplante, M.A., El Midaoui, A., Moreau, P., Lamontagne, D., de Champlain, J. J. Hypertens. (2003) [Pubmed]
  12. Omapatrilat and enalapril in patients with hypertension: the Omapatrilat Cardiovascular Treatment vs. Enalapril (OCTAVE) trial. Kostis, J.B., Packer, M., Black, H.R., Schmieder, R., Henry, D., Levy, E. Am. J. Hypertens. (2004) [Pubmed]
  13. Omapatrilat induces profound renal vasodilation but does not affect coronary hemodynamics. Varagic, J., Susic, D., Slama, M., Frohlich, E.D. J. Cardiovasc. Pharmacol. Ther. (2003) [Pubmed]
  14. The clinical, cardiac, renal, arterial and neurohormonal effects of omapatrilat, a vasopeptidase inhibitor, in patients with chronic heart failure. McClean, D.R., Ikram, H., Garlick, A.H., Richards, A.M., Nicholls, M.G., Crozier, I.G. J. Am. Coll. Cardiol. (2000) [Pubmed]
  15. Disposition and safety of omapatrilat in subjects with renal impairment. Sica, D.A., Liao, W., Gehr, T.W., Khan, S., Jemal, M., Delaney, C.L., Ferreira, I.M., Malhotra, B.K. Clin. Pharmacol. Ther. (2000) [Pubmed]
  16. In vitro and in vivo inhibition of the 2 active sites of ACE by omapatrilat, a vasopeptidase inhibitor. Azizi, M., Massien, C., Michaud, A., Corvol, P. Hypertension (2000) [Pubmed]
  17. Effect of vasopeptidase inhibitor omapatrilat on cardiomyocyte apoptosis and ventricular remodeling in rat myocardial infarction. Bäcklund, T., Palojoki, E., Saraste, A., Grönholm, T., Eriksson, A., Lakkisto, P., Vuolteenaho, O., Nieminen, M.S., Voipio-Pulkki, L.M., Laine, M., Tikkanen, I. Cardiovasc. Res. (2003) [Pubmed]
  18. Vasopeptidase inhibition with omapatrilat increases fluid and protein microvascular permeability in cat skeletal muscle. Persson, J., Morsing, P., Grände, P.O. J. Hypertens. (2004) [Pubmed]
  19. Bioenergetic protection of failing atrial and ventricular myocardium by vasopeptidase inhibitor omapatrilat. Cha, Y.M., Dzeja, P.P., Redfield, M.M., Shen, W.K., Terzic, A. Am. J. Physiol. Heart Circ. Physiol. (2006) [Pubmed]
  20. Protective effect of omapatrilat, a vasopeptidase inhibitor, on the metabolism of bradykinin in normal and failing human hearts. Blais, C., Fortin, D., Rouleau, J.L., Molinaro, G., Adam, A. J. Pharmacol. Exp. Ther. (2000) [Pubmed]
  21. Effect of dual angiotensin converting enzyme/neutral endopeptidase inhibition, angiotensin converting enzyme inhibition, or AT1 antagonism on coronary microvasculature in spontaneously hypertensive rats. Pu, Q., Larouche, I., Schiffrin, E.L. Am. J. Hypertens. (2003) [Pubmed]
  22. Pharmacodynamic effects of dual neutral endopeptidase-angiotensin-converting enzyme inhibition versus angiotensin-converting enzyme inhibition in humans. Massien, C., Azizi, M., Guyene, T.T., Vesterqvist, O., Mangold, B., Ménard, J. Clin. Pharmacol. Ther. (1999) [Pubmed]
  23. Systemic and renal effect of chronic omapatrilat in sodium-restricted, one-kidney, one-clip hypertensive rats. Jover, B., Stuit, L., Mimran, A. J. Hypertens. (2004) [Pubmed]
  24. Insulin stimulates endogenous angiotensin II production via a mitogen-activated protein kinase pathway in vascular smooth muscle cells. Tuck, M.L., Bounoua, F., Eslami, P., Nyby, M.D., Eggena, P., Corry, D.B. J. Hypertens. (2004) [Pubmed]
  25. Omapatrilat, a dual angiotensin-converting enzyme and neutral endopeptidase inhibitor, prevents fatty streak deposit in apolipoprotein E-deficient mice. Arnal, J.F., Castano, C., Maupas, E., Mugniot, A., Darblade, B., Gourdy, P., Michel, J.B., Bayard, F. Atherosclerosis (2001) [Pubmed]
  26. Chronic vasopeptidase inhibition restores endothelin-converting enzyme activity and normalizes endothelin levels in salt-induced hypertension. Quaschning, T., d'Uscio, L.V., Shaw, S., Viswambharan, H., Ruschitzka, F.T., Lüscher, T.F. Nephrol. Dial. Transplant. (2001) [Pubmed]
  27. Vasopeptidase inhibition: a new concept in blood pressure management. Burnett, J.C. Journal of hypertension. Supplement : official journal of the International Society of Hypertension. (1999) [Pubmed]
  28. Renoprotective effect of long-term combined treatment with adrenomedullin and omapatrilat in hypertensive rats. Ishimura, K., Nishikimi, T., Akimoto, K., Ono, H., Kangawa, K., Matsuoka, H. J. Hypertens. (2005) [Pubmed]
  29. Emerging treatments for hypertension: potential role for vasopeptidase inhibition. Weber, M. Am. J. Hypertens. (1999) [Pubmed]
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