enalaprilat

Summary

Summary: The active metabolite of ENALAPRIL and one of the potent, intravenously administered, ANGIOTENSIN-CONVERTING ENZYME INHIBITORS. It is an effective agent for the treatment of essential hypertension and has beneficial hemodynamic effects in heart failure. The drug produces renal vasodilation with an increase in sodium excretion.

Top Publications

  1. Rigol M, Heras M, Solanes N, Epelde F, Roig E, Perez Villa F, et al. Enalaprilat, losartan and LU 135252 in coronary blood flow regulation. Eur J Clin Invest. 2003;33:363-9 pubmed
    ..The pigs were distributed to: Group 1 (n = 7) angiotensin II; Group 2 (n = 7) enalaprilat + angiotensin II; Group 3 (n = 9) the bradykinin B2 antagonist HOE 140 + enalaprilat + angiotensin II; Group 4 (..
  2. Lee J, Son J, Lee M, Lee K, Kim D. Simultaneous quantitation of enalapril and enalaprilat in human plasma by 96-well solid-phase extraction and liquid chromatography/tandem mass spectrometry. Rapid Commun Mass Spectrom. 2003;17:1157-62 pubmed
    ..has been developed and validated for the quantitative determination of enalapril and its active metabolite enalaprilat in human plasma...
  3. Decarie A, Raymond P, Gervais N, Couture R, Adam A. Serum interspecies differences in metabolic pathways of bradykinin and [des-Arg9]BK: influence of enalaprilat. Am J Physiol. 1996;271:H1340-7 pubmed
    ..The in vitro incubation of BK and [des-Arg9]BK in the serum of four species with or without enalaprilat and the quantification of the immunoreactivity of both peptides at different time intervals allowed the ..
  4. Jablonskis L, Rogers P, Lungershausen Y, Howe P. Chronic central administration of enalaprilat lowers blood pressure in stroke-prone spontaneously hypertensive rats. J Auton Nerv Syst. 1992;39:119-26 pubmed
    ..The ACE inhibitor, enalaprilat, was infused i.c.v. for two weeks at a rate of 5 micrograms/h via osmotic minipumps...
  5. Gu Q, Chen X, Zhong D, Wang Y. Simultaneous determination of enalapril and enalaprilat in human plasma by liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2004;813:337-42 pubmed
    ..method was developed and validated for simultaneous determination of enalapril and its major active metabolite enalaprilat in human plasma...
  6. Andujar Sánchez M, Camara Artigas A, Jara Perez V. A calorimetric study of the binding of lisinopril, enalaprilat and captopril to angiotensin-converting enzyme. Biophys Chem. 2004;111:183-9 pubmed
    ..Nevertheless, a 1:1 stoichiometry for the binding of lisinopril, captopril or enalaprilat to somatic pig lung ACE is shown by isothermal titration calorimetry (ITC) and enzymatic assays...
  7. Natesh R, Schwager S, Evans H, Sturrock E, Acharya K. Structural details on the binding of antihypertensive drugs captopril and enalaprilat to human testicular angiotensin I-converting enzyme. Biochemistry. 2004;43:8718-24 pubmed
    ..structures of testis ACE (tACE) in complex with the first successfully designed ACE inhibitor captopril and enalaprilat, the Phe-Ala-Pro analogue...
  8. Ungi I, Palinkas A, Nemes A, Ungi T, Thury A, Sepp R, et al. Myocardial protection with enalaprilat in patients unresponsive to ischemic preconditioning during percutaneous coronary intervention. Can J Physiol Pharmacol. 2008;86:827-34 pubmed publisher
    ..The objective of the present study was to examine whether the administration of enalaprilat to these patients results in protection...
  9. Hamidi M, Tajerzadeh H, Dehpour A, Ejtemaee Mehr S. Inhibition of serum angiotensin-converting enzyme in rabbits after intravenous administration of enalaprilat-loaded intact erythrocytes. J Pharm Pharmacol. 2001;53:1281-6 pubmed
    ..time courses of serum angiotensin-converting enzyme (ACE) activity after intravenous administration of enalaprilat encapsulated in intact erythrocytes was evaluated and compared with free drug, in a rabbit model...

More Information

Publications93

  1. Mangiacapra F, Peace A, Di Serafino L, Pyxaras S, Bartunek J, Wyffels E, et al. Intracoronary EnalaPrilat to Reduce MICROvascular Damage During Percutaneous Coronary Intervention (ProMicro) study. J Am Coll Cardiol. 2013;61:615-21 pubmed publisher
    This study investigated the influence of intracoronary enalaprilat on coronary microvascular function and peri-procedural outcome measures in patients with stable angina undergoing percutaneous coronary intervention (PCI)...
  2. Kim K, Kim S, Yang C, Li C, Chung Y, Lee S, et al. Differentiation between acute cyclosporine nephrotoxicity and acute tubular necrosis using enalaprilat renal scintigraphy in rats. Invest Radiol. 2003;38:473-81 pubmed
    ..The purpose of this study was to differentiate acute CsA nephrotoxicity from ATN using enalaprilat renal scintigraphy in rats...
  3. Leesar M, Jneid H, Tang X, Bolli R. Pretreatment with intracoronary enalaprilat protects human myocardium during percutaneous coronary angioplasty. J Am Coll Cardiol. 2007;49:1607-10 pubmed
    We tested the hypothesis that enalaprilat induces preconditioning (PC)-mimetic actions in patients with stable coronary artery disease...
  4. Salgado D, He X, Su F, de Sousa D, Penaccini L, Maciel L, et al. Sublingual microcirculatory effects of enalaprilat in an ovine model of septic shock. Shock. 2011;35:542-9 pubmed publisher
    ..serum angiotensin II levels may play a role in this dysfunction, we evaluated the microcirculatory effects of enalaprilat in an experimental model of septic shock. One hour after injection of 1...
  5. Ahlin P, Kristl J, Kristl A, Vrecer F. Investigation of polymeric nanoparticles as carriers of enalaprilat for oral administration. Int J Pharm. 2002;239:113-20 pubmed
    b>Enalaprilat is a typical angiotensin-converting enzyme inhibitor and is very poorly absorbed from the gastrointestinal tract...
  6. Varon J, Marik P. The diagnosis and management of hypertensive crises. Chest. 2000;118:214-27 pubmed
    ..This article reviews some of the current concepts and common misconceptions in the management of patients with acutely elevated BP...
  7. Yu M, Zheng Y, Sun H, Yu D. Inhibitory effects of enalaprilat on rat cardiac fibroblast proliferation via ROS/P38MAPK/TGF-?1 signaling pathway. Molecules. 2012;17:2738-51 pubmed publisher
    b>Enalaprilat (Ena...
  8. Hirschl M, Binder M, Bur A, Herkner H, Brunner M, Mullner M, et al. Clinical evaluation of different doses of intravenous enalaprilat in patients with hypertensive crises. Arch Intern Med. 1995;155:2217-23 pubmed
    The appropriate dose of intravenous enalaprilat to be used in the treatment of hypertensive crisis is controversial...
  9. Lu S, Jiang K, Qin F, Lu X, Li F. Simultaneous quantification of enalapril and enalaprilat in human plasma by high-performance liquid chromatography-tandem mass spectrometry and its application in a pharmacokinetic study. J Pharm Biomed Anal. 2009;49:163-7 pubmed publisher
    ..mass spectrometry (HPLC-MS/MS) method was developed to simultaneously determine enalapril and enalaprilat in human plasma...
  10. Hamidi M, Tajerzadeh H, Dehpour A, Rouini M, Ejtemaee Mehr S. In vitro characterization of human intact erythrocytes loaded by enalaprilat. Drug Deliv. 2001;8:223-30 pubmed
    In vitro characteristics of the human erythrocytes loaded by enalaprilat have been evaluated...
  11. Trapp O, Trapp G, Schurig V. Determination of the cis-trans isomerization barrier of enalaprilat by dynamic capillary electrophoresis and computer simulation. Electrophoresis. 2004;25:318-23 pubmed
    ..model has been applied to determine the isomerization barriers of the angiotensin converting enzyme inhibitor enalaprilat. The separation of the rotational cis-trans isomeric drug has been performed in an aqueous 20 mM borate buffer ..
  12. Lupi R, Del Guerra S, Bugliani M, Boggi U, Mosca F, Torri S, et al. The direct effects of the angiotensin-converting enzyme inhibitors, zofenoprilat and enalaprilat, on isolated human pancreatic islets. Eur J Endocrinol. 2006;154:355-61 pubmed
    ..2 mmol/l glucose, with or without the presence in the incubation medium of 0.5-6.0 mmol/l zofenoprilat or enalaprilat, ACE inhibitor drugs which differ by the presence of a sulphydryl or a carboxyl group in their structural ..
  13. Mühlen B, Millgard J, Lind L. Effects of digoxin, furosemide, enalaprilat and metoprolol on endothelial function in young normotensive subjects. Clin Exp Pharmacol Physiol. 2001;28:381-5 pubmed
    ..1 mg/h), furosemide (5.0 mg/h), enalaprilat (2,4 mg/h), metoprolol (1.2 mg/h) or saline (controls). 3...
  14. Muir W, Sams R, Hubbell J, Hinchcliff K, Gadawski J. Effects of enalaprilat on cardiorespiratory, hemodynamic, and hematologic variables in exercising horses. Am J Vet Res. 2001;62:1008-13 pubmed
    To determine the effects of IV administration of enalaprilat on cardiorespiratory and hematologic variables as well as inhibition of angiotensin converting enzyme (ACE) activity in exercising horses. 6 adult horses...
  15. Fujioka H, Hieda Y, Kuramoto Y, Konishi K, Kinoshita Kikuta E, Kinoshita E, et al. [Increase in lipophilicity of enalaprilat by complexation with copper(II) or zinc(II) Ions]. Yakugaku Zasshi. 2013;133:1135-41 pubmed
    b>Enalaprilat (H2L), which is the active metabolite of the pro-drug enalapril, is an angiotensin-converting enzyme inhibitor...
  16. Morano S, Cipriani R, Cerrito M, Santangelo C, Vasaturo F, Pantellini F, et al. Angiotensin-converting enzyme inhibition modulates high-glucose-induced extracellular matrix changes in mouse glomerular epithelial cells. Nephron Exp Nephrol. 2003;95:e30-5 pubmed
    ..Glomerular epithelial cells were cultured in 5 and 30 mmol/l glucose, with and without enalaprilat (0.3 mmol/l)...
  17. Kingma J, Simard D, Rouleau J. Modulation of nitric oxide affects myocardial perfusion-contraction matching in anaesthetized dogs with recurrent no-flow ischaemia. Exp Physiol. 2011;96:1293-301 pubmed publisher
    ..The following three groups were studied: (1) saline; (2) L-NAME (10 mg kg(-1) I.V.); and (3) enalaprilat (1.5 mg kg(-1) I.V.)...
  18. Ruan X, Wagner C, Chatziantoniou C, Kurtz A, Arendshorst W. Regulation of angiotensin II receptor AT1 subtypes in renal afferent arterioles during chronic changes in sodium diet. J Clin Invest. 1997;99:1072-81 pubmed
    ..56% decrease in renal blood flow, P < 0.001). After acute blockade of ANG II formation by iv enalaprilat injection in sodium-restricted animals, ANG II produced a 40% decrease in renal blood flow, a level between ..
  19. Petrov M, Shilo V, Tarasov A, Schwartz D, Garcia J, Kost O, et al. Conformational changes of blood ACE in chronic uremia. PLoS ONE. 2012;7:e49290 pubmed publisher
    ..The pattern of binding of monoclonal antibodies (mAbs) to 16 epitopes on human angiotensin I-converting enzyme (ACE) comprise a conformational ACE fingerprint and is a sensitive marker of subtle protein conformational changes...
  20. Visscher C, de Zeeuw D, de Jong P, Piers D, Beekhuis H, Groothuis G, et al. Angiotensin-converting enzyme inhibition-induced changes in hippurate renography and renal function in renovascular hypertension. J Nucl Med. 1996;37:482-8 pubmed
    ..We studied the mechanism of angiotensin-converting enzyme (ACE) inhibition-induced changes in hippurate renography of the poststenotic kidney...
  21. Wall P, Buising C, Henderson L, Rickers T, Cárdenas A, Owens L, et al. Enalaprilat improves systemic cardiovascular parameters and mesenteric blood flow during hypotensive resuscitation from hemorrhagic shock in dogs. Shock. 2002;17:228-33 pubmed
    ..Blocking angiotensin II formation with enalaprilat may be such an intervention...
  22. Kijtawornrat A, Ozkanlar Y, Keene B, Roche B, Hamlin D, Hamlin R. Assessment of drug-induced QT interval prolongation in conscious rabbits. J Pharmacol Toxicol Methods. 2006;53:168-73 pubmed
    ..cisapride, dofetilide and haloperidol), two drugs known to be non-torsadogenic in humans (propranolol and enalaprilat) and a control article (vehicle)...
  23. Lazar H, Bao Y, Rivers S, Colton T, Bernard S. High tissue affinity angiotensin-converting enzyme inhibitors improve endothelial function and reduce infarct size. Ann Thorac Surg. 2001;72:548-53; discussion 553-4 pubmed
    ..During the period of coronary occlusion, 10 pigs received enalaprilat (low affinity tissue ACE inhibitor), 0...
  24. Adler A, Messina E, Sherman B, Wang Z, Huang H, Linke A, et al. NAD(P)H oxidase-generated superoxide anion accounts for reduced control of myocardial O2 consumption by NO in old Fischer 344 rats. Am J Physiol Heart Circ Physiol. 2003;285:H1015-22 pubmed
    ..70 +/- 0.02 to 0.90 +/- 0.02 g). The NO-mediated control of cardiac O2 consumption by bradykinin or enalaprilat was not different between 4 mo (36 +/- 2 or 34 +/- 3%) and 14 mo (29 +/- 1 or 25 +/- 3%) but markedly (P < 0...
  25. Pretorius M, Rosenbaum D, Vaughan D, Brown N. Angiotensin-converting enzyme inhibition increases human vascular tissue-type plasminogen activator release through endogenous bradykinin. Circulation. 2003;107:579-85 pubmed
    ..We measured the effect of intra-arterial enalaprilat (5 micro g/min) on forearm blood flow (FBF) and net t-PA release before and during intra-arterial infusion of ..
  26. Ghosh C, Jain I, Shinde C, Chakraborty B. Rapid and sensitive liquid chromatography/tandem mass spectrometry method for simultaneous determination of enalapril and its major metabolite enalaprilat, in human plasma: application to a bioequivalence study. Drug Test Anal. 2012;4:94-103 pubmed publisher
    A rapid and most sensitive method for simultaneous determination of enalapril (ENP) and its metabolite, enalaprilat (ENPT), in human plasma using ESI-LC-MS/MS (electrospray ionization liquid chromatography tandem mass spectrometry) ..
  27. Mohri M, Tagawa H, Egashira K, Takeshita A. Intracoronary enalaprilat improves metabolic coronary vasodilation in patients with idiopathic dilated cardiomyopathy. J Cardiovasc Pharmacol. 2000;35:249-55 pubmed
    ..We examined acute effects of intracoronary enalaprilat on metabolic coronary vasodilation during pacing tachycardia in patients...
  28. Xiao R, Huang Y, Lei Z, Ruan J. [Effects of single or combined administration of cedilanid and enalaprilat on visceral damages in early stage of severe scald in rats]. Zhonghua Shao Shang Za Zhi. 2008;24:428-31 pubmed
    To investigate the effects of single or combined administration of cedilanid and small-dose of enalaprilat on heart, liver, kidney and intestine damages at early stage of severe scald in rats...
  29. Kocijan A, Grahek R, Kocjan D, Zupancic Kralj L. Effect of column temperature on the behaviour of some angiotensin converting enzyme inhibitors during high-performance liquid chromatographic analysis. J Chromatogr B Biomed Sci Appl. 2001;755:229-35 pubmed
    The chromatographic behaviour of the ACE inhibitors lisinopril, enalapril and its two degradation products, enalaprilat (hydrolytic degradation product) and diketopiperazine (DKP) (cyclization degradation product) was studied as a ..
  30. Handrakis J, DeMeersman R, Rosado Rivera D, LaFountaine M, Spungen A, Bauman W, et al. Effect of hypotensive challenge on systemic hemodynamics and cerebral blood flow in persons with tetraplegia. Clin Auton Res. 2009;19:39-45 pubmed publisher
    ..25 mg enalaprilat) and 45 degrees head-up tilt (HUT)...
  31. Redublo Quinto B, Camargo de Andrade M, Ronchi F, Santos E, Alves Correa S, Shimuta S, et al. Expression of angiotensin I-converting enzymes and bradykinin B2 receptors in mouse inner medullary-collecting duct cells. Int Immunopharmacol. 2008;8:254-60 pubmed publisher
    ..Captopril and enalaprilat inhibited the purified enzymes...
  32. van der Giet M, Erinola M, Zidek W, Tepel M. Captopril and quinapril reduce reactive oxygen species. Eur J Clin Invest. 2002;32:732-7 pubmed
    ..The effects of quinaprilat, captopril, enalaprilat and lisinopril on phorbol myristate acetate-induced reactive oxygen species generation were investigated in ..
  33. Turkyilmaz S, Alhan E, Ercin C, Vanizor B. Effects of enalaprilat on acute necrotizing pancreatitis in rats. Inflammation. 2007;30:205-12 pubmed
    The aim of this study was to investigate the influence of enalaprilat on acute necrotizing pancreatitis (ANP) induced by glycodeoxycholic acid in rats...
  34. Okuyama C, Mendes G, Faro R, Rezende V, Lagos R, Astigarraga R, et al. Pharmacokinetics and pharmacodynamics of a nitric oxide-releasing derivative of enalapril in male beagles. Clin Exp Pharmacol Physiol. 2007;34:290-5 pubmed
    ..18 +/- 4.72, 229.37 +/- 51.32 and 5159.23 +/- 514.88 microg.h/L for the analytes nitro-enalapril, enalapril and enalaprilat, respectively. In the enalapril group, the AUC(0-24h) was 704.53 +/- 158.86 and 4149.27 +/- 847.30 microg...
  35. Jover B, Dupont M, Mimran A, Woods R, McGrath B. Vasoconstrictor role for vasopressin in conscious, sodium-depleted rats. Am J Physiol. 1987;253:H763-9 pubmed
    ..were performed after selective or combined blockade with the vasopressin antagonist [d(CH2)5Tyr(Me)]AVP (AVPA), enalaprilat (CEI), and phentolamine (PHENTOL)...
  36. Chauhan V, Negi R, Sharma A, Gupta S, Mokta J, Verma B, et al. Enalaprilat induced acute parotitis. J Assoc Physicians India. 2008;56:128-9 pubmed
    ..There is no case of acute bilateral parotitis reported previously with i.v. enalaprilat. We present here a female patient who developed acute bilateral parotitis within minutes of i.v...
  37. Wells T, Rippley R, Hogg R, Sakarcan A, Blowey D, Walson P, et al. The pharmacokinetics of enalapril in children and infants with hypertension. J Clin Pharmacol. 2001;41:1064-74 pubmed
    ..Serum concentrations of enalaprilat, the active metabolite of enalapril, peaked between 4 and 6 hours after the first dose and 3 and 4 hours after ..
  38. Jackson K, Marques F, Watson A, Palma Rigo K, Nguyen Huu T, Morris B, et al. A novel interaction between sympathetic overactivity and aberrant regulation of renin by miR-181a in BPH/2J genetically hypertensive mice. Hypertension. 2013;62:775-81 pubmed publisher
    ..p.) in mice pretreated with the angiotensin-converting enzyme inhibitor enalaprilat (1.5 mg/kg i.p...
  39. Van Guilder G, Pretorius M, Luther J, Byrd J, Hill K, Gainer J, et al. Bradykinin type 2 receptor BE1 genotype influences bradykinin-dependent vasodilation during angiotensin-converting enzyme inhibition. Hypertension. 2008;51:454-9 pubmed publisher
    ..in 89 normotensive, nonsmoking, white American subjects in whom degradation of bradykinin was blocked by enalaprilat. BE1 genotype frequencies were +9/+9:+9/-9:-9/-9=19:42:28...
  40. Riou L, Ruiz M, Rieger J, Macdonald T, Watson D, Linden J, et al. Influence of propranolol, enalaprilat, verapamil, and caffeine on adenosine A(2A)-receptor-mediated coronary vasodilation. J Am Coll Cardiol. 2002;40:1687-94 pubmed
    The study was done to determine the effects of propranolol, enalaprilat, verapamil, and caffeine on the vasodilatory properties of the adenosine A(2A)-receptor agonist ATL-146e (ATL)...
  41. Denton K, Shweta A, Flower R, Anderson W. Predominant postglomerular vascular resistance response to reflex renal sympathetic nerve activation during ANG II clamp in rabbits. Am J Physiol Regul Integr Comp Physiol. 2004;287:R780-6 pubmed
    ..One group (ANG II clamp) received an infusion of an angiotensin-converting enzyme inhibitor (enalaprilat, 2 mg/kg bolus plus 2 mg.kg(-1).h(-1)) plus ANG II ( approximately 20 ng.kg(-1).min(-1)), the other vehicle...
  42. Lei Z, Huang Y, Xiao R, Zhang B, Zhang Q. [Effects of angiotensin (1-7) and enalaprilat on function of isolated rat heart perfused by burn serum]. Zhonghua Shao Shang Za Zhi. 2009;25:180-3 pubmed
    To investigate effects of angiotensin (1-7) [Ang (1-7)] and enalaprilat on function of isolated rat heart perfused by burn serum. Eighty SD rats were used to prepare burn serum...
  43. Lindsey C, Bendhack L, Paiva A. Effects of teprotide, captopril and enalaprilat on arterial wall kininase and angiotensin converting activity. J Hypertens Suppl. 1987;5:S71-6 pubmed
    ..More recently, we showed that conversion of ANG I in the perfused mesenteric vascular bed was not inhibited by enalaprilat at concentrations above those which maximally inhibited kininase activity...
  44. Li D, Xu S, Wang Y, Li D, Li X, Pan J, et al. Pharmacokinetics and drug-drug interaction between enalapril, enalaprilat and felodipine extended release (ER) in healthy subjects. Oncotarget. 2017;8:70752-70760 pubmed publisher
    ..Although the difference in PK parameters was statistically significant, its clinical significance may be limited, considering safety profile observed in the present study...
  45. Wittstein I, Kass D, Pak P, Maughan W, Fetics B, Hare J. Cardiac nitric oxide production due to angiotensin-converting enzyme inhibition decreases beta-adrenergic myocardial contractility in patients with dilated cardiomyopathy. J Am Coll Cardiol. 2001;38:429-35 pubmed
    ..The hemodynamic responses to intravenous dobutamine were determined before and during intracoronary infusion of enalaprilat (0.2 mg/min) with and without the NOS inhibitor N(G)-monomethyl-L-arginine (L-NMMA, 5 mg/min)...
  46. van Onzenoort H, Bussink M, Menheere P, van Mook W, van der Kuy P. The effect of sublingual captopril versus intravenous enalaprilat on angiotensin II plasma levels. Pharm World Sci. 2006;28:131-4 pubmed
    ..Because enteral administration of drugs was impossible, intravenous enalaprilat 2 mg once a day for 1 day followed by sublingual captopril 25 mg twice a day were started...
  47. Ramusovic S, Laeer S. An integrated physiology-based model for the interaction of RAA system biomarkers with drugs. J Cardiovasc Pharmacol. 2012;60:417-28 pubmed publisher
    ..Next, a physiology-based PK model for enalapril and enalaprilat was developed and coupled to the RAAS model...
  48. Palm F, Connors S, Mendonca M, Welch W, Wilcox C. Angiotensin II type 2 receptors and nitric oxide sustain oxygenation in the clipped kidney of early Goldblatt hypertensive rats. Hypertension. 2008;51:345-51 pubmed
    ..blood flow, and renal cortical oxygen tension (Po(2)) were measured after acute administration of an ACEI (enalaprilat) and after acute administration of ACEI following acute administration of an angiotensin II type 1 or ..
  49. Padilha A, Rossoni L, Xavier F, Vassallo D. Ouabain at nanomolar concentration promotes synthesis and release of angiotensin II from the endothelium of the tail vascular bed of spontaneously hypertensive rats. J Cardiovasc Pharmacol. 2004;44:372-80 pubmed
    ..05). In SHR/E+, pretreatment with losartan (10 microM) or enalaprilat (1 microM) prevented the increased sensitivity to PHE induced by OUA...
  50. Takimoto M, Mitani H, Hori S, Kimura M, Bandoh T, Okada T. Expression, secretion, and inhibition of angiotensin-converting enzyme in cultured human bronchial epithelial cells. Eur J Pharmacol. 1999;370:169-77 pubmed
    ..Angiotensin-converting enzyme inhibitors (imidaprilat, enalaprilat) inhibited the enzyme activity in bronchial epithelial cells with an IC50 of 0.9-3.6 nM...
  51. Ramusovic S, Thielking G, Laer S. Determination of enalapril and enalaprilat in small human serum quantities for pediatric trials by HPLC-tandem mass spectrometry. Biomed Chromatogr. 2012;26:697-702 pubmed publisher
    The angiotensin converting enzyme-inhibitor enalapril is the prodrug of enalaprilat and used in the treatment pediatric hypertension and chronic heart failure...
  52. Rouine Rapp K, Mello D, Hanley F, Mohan Reddy V, Soifer S. Effect of enalaprilat on postoperative hypertension after surgical repair of coarctation of the aorta. Pediatr Crit Care Med. 2003;4:327-32 pubmed
    ..The renin-angiotensin system mediates at least part of this hypertension. Enalaprilat, the only intravenous angiotensin-converting enzyme inhibitor, is used to treat hypertension in pediatric ..
  53. Weaver Osterholtz D, Reams G, De Vergel C, Bauer J. The bladder angiotensin system in female rats: response to infusions of angiotensin I and the angiotensin converting enzyme inhibitor enalaprilat. J Urol. 2001;165:1735-8 pubmed
    ..Each was given an intravenous bolus infusion of ANG I, the ANG converting enzyme inhibitor enalaprilat or saline...
  54. Gobeil F, Hallé S, Blais P, Regoli D. Studies on the angiotensin-converting enzyme and the kinin B2 receptor in the rabbit jugular vein: modulation of contractile response to bradykinin. Can J Physiol Pharmacol. 2002;80:153-63 pubmed
    ..ACE-I (captopril, enalaprilat) were unable to prevent B2 receptor desensitisation induced by BK (1 microM)...
  55. Borba M, Lopes R, Carmona M, Neto B, Nahas S, Pereira P. Effects of enalaprilat on the renin-angiotensin-aldosterone system and on renal function during CO2 pneumoperitoneum. J Endourol. 2005;19:1026-31 pubmed
    ..The aim of this study was to evaluate the effects of enalaprilat (Vasotec) administration on renal function during CO2 pneumoperitoneum, given that this drug, which is an ..
  56. Andrawis N, Dzau V, Pratt R. Autocrine stimulation of mas oncogene leads to altered growth control. Cell Biol Int Rep. 1992;16:547-56 pubmed
    ..Our results suggest that the transformed phenotype is due to the production of a mas receptor ligand distinct from angiotensin. ..
  57. Quan A, Baum M. The renal nerve is required for regulation of proximal tubule transport by intraluminally produced ANG II. Am J Physiol Renal Physiol. 2001;280:F524-9 pubmed
    ..The decrement in volume reabsorption after addition of 10(-4) M luminal enalaprilat is a measure of the role of luminal angiotensin II on transport...
  58. Fallet R, Bast J, Fujiwara K, Ishii N, Sansom S, Carmines P. Influence of Ca(2+)-activated K(+) channels on rat renal arteriolar responses to depolarizing agonists. Am J Physiol Renal Physiol. 2001;280:F583-91 pubmed
    ..These observations suggest that the BK(Ca) channels evident in afferent arteriolar smooth muscle do not provide a prominent physiological brake on agonist-induced constriction under our experimental conditions. ..
  59. Wiggers G, Stefanon I, Padilha A, Peçanha F, Vassallo D, Oliveira E. Low nanomolar concentration of mercury chloride increases vascular reactivity to phenylephrine and local angiotensin production in rats. Comp Biochem Physiol C Toxicol Pharmacol. 2008;147:252-60 pubmed
    ..This response is endothelium mediated and involves the reduction of NO bioavailability and the action of reactive oxygen species. The local ACE participates in mercury actions and depends on the angiotensin II generation...
  60. Parrish J, Amundson D. Is there an "ACE" in the hole for postcoronary artery bypass graft myocardial dysfunction?. Crit Care Med. 2003;31:1591 pubmed
  61. De Mello W, Monterrubio J. Intracellular and extracellular angiotensin II enhance the L-type calcium current in the failing heart. Hypertension. 2004;44:360-4 pubmed
    ..enhanced the peak I(Ca) density and the rate of I(Ca) inactivation, an effect that was reduced by intracellular enalaprilat (10(-8) mmol/L). Moreover, intracellular enalaprilat by itself reduced the peak I(Ca) density...
  62. Sueyoshi R, Ignatoski K, Daignault S, Okawada M, Teitelbaum D. Angiotensin converting enzyme-inhibitor reduces colitis severity in an IL-10 knockout model. Dig Dis Sci. 2013;58:3165-77 pubmed publisher
    ..Colitis was induced by giving 10-week old IL-10-/- mice piroxicam (P.O.) for 14 days. The ACE-I enalaprilat was given transanally at a dose of 6.25 mg/kg for 21 days...
  63. Marwood J. Effect of angiotensin II receptor blockade on the interaction between enalaprilat and doxazosin in rat tail arteries. Clin Exp Pharmacol Physiol. 1998;25:517-21 pubmed
    1. Previous work has shown that enalaprilat, an inhibitor of angiotensin-converting enzyme (ACE), potentiated the actions of alpha 1-adrenoceptor antagonists; it was hypothesized that angiotensin II (AngII) modulated the activity of ..
  64. Norman J, Stidwill R, Singer M, Fine L. Angiotensin II blockade augments renal cortical microvascular pO2 indicating a novel, potentially renoprotective action. Nephron Physiol. 2003;94:p39-46 pubmed
    ..Animals received non-hypotensive doses of enalaprilat (100 microg/kg i.v.) or candesartan (40 microg/kg i.v...
  65. O Tierney P, Anderson D, Faber J, Louey S, Thornburg K, Giraud G. Reduced systolic pressure load decreases cell-cycle activity in the fetal sheep heart. Am J Physiol Regul Integr Comp Physiol. 2010;299:R573-8 pubmed publisher
    ..Sixteen fetal sheep were given either continuous intravenous infusion of lactated Ringer solution (LR) or enalaprilat, an angiotensin-converting enzyme inhibitor beginning at 127 days gestational age...
  66. Zou K, Maeda T, Watanabe A, Liu J, Liu S, Oba R, et al. Abeta42-to-Abeta40- and angiotensin-converting activities in different domains of angiotensin-converting enzyme. J Biol Chem. 2009;284:31914-20 pubmed publisher
  67. Varon J, Marik P. Perioperative hypertension management. Vasc Health Risk Manag. 2008;4:615-27 pubmed
    ..When treatment is necessary, therapy should be individualized for the patient. This paper reviews the pharmacologic agents and strategies commonly used in the management of perioperative hypertension. ..
  68. Pretorius M, Van Guilder G, Guzman R, Luther J, Brown N. 17Beta-estradiol increases basal but not bradykinin-stimulated release of active t-PA in young postmenopausal women. Hypertension. 2008;51:1190-6 pubmed publisher
    ..methacholine, and nitroprusside on forearm blood flow and net t-PA release, before and during intraarterial enalaprilat (0.33 microg/min/100 mL forearm volume)...
  69. Nikolaidis L, Doverspike A, Huerbin R, Hentosz T, Shannon R. Angiotensin-converting enzyme inhibitors improve coronary flow reserve in dilated cardiomyopathy by a bradykinin-mediated, nitric oxide-dependent mechanism. Circulation. 2002;105:2785-90 pubmed
    ..The purpose of the present study was to determine the effects and the mechanism of action of the ACE inhibitor enalaprilat and the AT1 antagonist losartan on regional myocardial perfusion and coronary flow and vasodilator reserve in ..
  70. Xu Y, Kumar D, Dyck J, Ford W, Clanachan A, Lopaschuk G, et al. AT(1) and AT(2) receptor expression and blockade after acute ischemia-reperfusion in isolated working rat hearts. Am J Physiol Heart Circ Physiol. 2002;282:H1206-15 pubmed
    ..5 micromol/l as positive control), enalaprilat (an ANG-converting enzyme inhibitor; 1 micromol/l), PD-123319 + losartan, ANG II (1 nmol/l), or ANG II + ..
  71. Bonnemeier H, Schäfer U, Kurz T, Ortak J, Hartmann F, Katus H, et al. Effects of intracoronary low-dose enalaprilat on ventricular repolarization dynamics after direct percutaneous intervention for acute myocardial infarction. Pacing Clin Electrophysiol. 2007;30:631-7 pubmed
    ..c.) application of enalaprilat (EN) as an adjunct to direct primary coronary intervention (PCI) on QT dynamics in the acute phase of MI...
  72. Roy C, Marceau E, Gera L, Marceau F. An in vitro reconstitution system to address the mechanism of the vascular expression of the bradykinin B? receptor in response to angiotensin converting enzyme inhibition. Vascul Pharmacol. 2012;57:15-23 pubmed publisher
    ..To identify cytokine-dependent or -independent mechanisms for the latter phenomenon, the ACE inhibitor enalaprilat and several peptides potentiated in vivo by ACE blockade were applied either directly to human umbilical artery ..
  73. Ramalho F, Ramalho L, Castro e Silva Junior O, Zucoloto S, Correa F. Effect of angiotensin-converting enzyme inhibitors on liver regeneration in rats. Hepatogastroenterology. 2002;49:1347-51 pubmed
    ..Adult rats received lisinopril, captopril, enalaprilat, or saline solution, intraperitoneally, for 5 days before 70% partial hepatectomy, and daily after surgery...
  74. Wang W, Xiao W, Sun L, Zhang C, Chen G, Yang H. Inhibition of ACE activity contributes to the intestinal structural compensation in a massive intestinal resection rat model. Pediatr Surg Int. 2012;28:533-41 pubmed publisher
    ..transection (n = 6); (2) Sham + ACE-I group received an ileum transaction and lavage with ACE inhibitor (ACE-I, enalaprilat, 2 mg/kg/day) (n = 6); (3) SBS group received a 70 % mid-intestinal resection (n = 6); (4) SBS + ACE-I group ..
  75. Imig J, Navar G, Zou L, O Reilly K, Allen P, Kaysen J, et al. Renal endosomes contain angiotensin peptides, converting enzyme, and AT(1A) receptors. Am J Physiol. 1999;277:F303-11 pubmed
    ..5-fold higher than the levels observed in renal endosomes. Acute enalaprilat treatment decreased ACE activity in renal intermicrovillar clefts by 90% and in renal endosomes by 84%...
  76. Mukhametova L, Gulin D, Binevskiĭ P, Aisina R, Kost O, Nikol skaia I. [The in vitro cross-effects of inhibitors of renin-angiotensin and fibrinolytic systems on the key enzymes of these systems]. Bioorg Khim. 2008;34:471-8 pubmed
    ..The data demonstrate that, along with endogenous mediated interactions, relations based on the direct interactions of exogenous inhibitors of one system affecting the activities of components of another system can take place. ..
  77. Gardner S, Atkins C, Sams R, Schwabenton A, Papich M. Characterization of the pharmacokinetic and pharmacodynamic properties of the angiotensin-converting enzyme inhibitor, enalapril, in horses. J Vet Intern Med. 2004;18:231-7 pubmed
    ..5 mg/kg PO) in 5 mares were investigated. After single i.v. dosing, concentrations of enalapril and enalaprilat, its active metabolite, were measured. Two weeks later, enalapril was administered by nasogastric tube...
  78. De Mello W. Further studies on the effect of intracellular angiotensins on heart cell communication: on the role of endogenous angiotensin II. Regul Pept. 2003;115:31-6 pubmed
    ..the influence of endogenous angiotensin II on the regulation of cell coupling, enalapril maleate (10(-8) M) or enalaprilat (10(-9) M) was used...
  79. Lee K, Yoo S, Holtby H, Grant B, Mroczek D, Wong D, et al. Acute effects of the ACE inhibitor enalaprilat on the pulmonary, cerebral and systemic blood flow and resistance after the bidirectional cavopulmonary connection. Heart. 2011;97:1343-8 pubmed publisher
    ..8 kg) undergoing a pre-Fontan catheterisation with MRI measurement of flows. Intravenous enalaprilat 0.005 or 0.01 mg/kg. Enalaprilat increased descending aorta flow (median 21.6%, p=0...
  80. Brovkovych V, Zhang Y, Brovkovych S, Minshall R, Skidgel R. A novel pathway for receptor-mediated post-translational activation of inducible nitric oxide synthase. J Cell Mol Med. 2011;15:258-69 pubmed publisher
    ..Angiotensin converting enzyme inhibitor enalaprilat also directly activated B1Rs to generate high output nitric oxide via the same pathway...
  81. Oosting J, Struijker Boudier H, Janssen B. Timed inhibition of the renin-angiotensin system suppresses the rise in blood pressure upon awakening in spontaneously hypertensive rats. Am J Hypertens. 1999;12:1109-18 pubmed
    ..efficacy of the angiotensin converting enzyme (ACE) inhibitors captopril (doses: 3, 10, and 30 mg/ kg/6 h) and enalaprilat (0.3 mg/kg/6 h), and the AT1-receptor antagonist losartan (10 mg/kg/6 h) at two different treatment regimens...
  82. Petrie M, Padmanabhan N, McDonald J, Hillier C, Connell J, McMurray J. Angiotensin converting enzyme (ACE) and non-ACE dependent angiotensin II generation in resistance arteries from patients with heart failure and coronary heart disease. J Am Coll Cardiol. 2001;37:1056-61 pubmed
    ..I (AI) and AII were constructed in the presence of 1) vehicle, 2) chymostatin [an inhibitor of chymase], 3) enalaprilat, and 4) the combination of chymostatin and enalaprilat...
  83. Miyamoto H, Ito K, Wakabayashi S, Suzaka H, Matsuo H, Iga T, et al. Comparative study of effects of angiotensin II receptor antagonist, KD3-671, and angiotensin converting enzyme inhibitor, enalaprilat, on cough reflex in guinea pig. Eur J Drug Metab Pharmacokinet. 2001;26:47-52 pubmed
    ..pharmacokinetics and cough-inducing effect of this drug in guinea-pig, compared with that of an ACE inhibitor, enalaprilat. KD3-671 was not significantly different from the vehicle treatment in the ability to induce coughing, whereas ..
  84. Dariolli R, Naghetini M, Marques E, Takimura C, Jensen L, Kiers B, et al. Allogeneic pASC transplantation in humanized pigs attenuates cardiac remodeling post-myocardial infarction. PLoS ONE. 2017;12:e0176412 pubmed publisher