Page last updated: 2024-12-06

quinapril

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Description

Quinapril is an angiotensin-converting enzyme (ACE) inhibitor used to treat high blood pressure (hypertension) and heart failure. It is a synthetically produced compound. Quinapril works by blocking the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor. This blockage leads to vasodilation (widening of blood vessels) and a decrease in blood pressure. Quinapril is also effective in reducing the risk of cardiovascular events, such as heart attack and stroke, in patients with high blood pressure. It is studied extensively due to its effectiveness and relative safety profile. Quinapril is well-tolerated by most patients and has a long half-life, allowing for once-daily dosing. It is a widely prescribed medication and plays a significant role in managing hypertension and heart failure.'

Quinapril: A tetrahydroisoquinoline derivative and ANGIOTENSIN CONVERTING ENZYME inhibitor that is used in the treatment of HYPERTENSION and HEART FAILURE. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

quinapril : A member of the class of isoquinolines that is (3S)-2-L-alanyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid in which the alpha-amino group of the alanyl residue has been substituted by a 1-ethoxycarbonyl-4-phenylbutan-2-yl group (the all-S isomer). A prodrug for quinaprilat (by hydrolysis of the ethyl ester to the corresponding carboxylic acid), it is used as an angiotensin-converting enzyme inhibitor (ACE inhibitor) used (generally as the hydrochloride salt) for the treatment of hypertension and congestive heart failure. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID54892
CHEMBL ID1592
CHEBI ID8713
SCHEMBL ID15813
MeSH IDM0122104

Synonyms (76)

Synonym
BIDD:GT0797
AB00053714-07
BRD-K72222507-003-03-6
quinaprilum
CHEBI:8713 ,
(3s)-2-{(2s)-2-[(1s)-1-ethoxycarbonyl-3-phenylpropylamino]propanoyl}-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
(3s)-2-{n-[(2s)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]-l-alanyl}-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
(3s)-2-{n-[(2s)-1-ethoxycarbonyl-4-phenylbutan-2-yl]-l-alanyl}-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
KBIO1_000710
DIVK1C_000710
(3s)-2-(n-{(1s)-1-[(ethyloxy)carbonyl]-3-phenylpropyl}-l-alanyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
quinapril (inn)
D03752
SPECTRUM_001597
SPECTRUM5_001075
quinapril
C07398
85441-61-8
DB00881
3-isoquinolinecarboxylic acid, 2-(2-((1-(ethoxycarbonyl)-3-phenylpropyl)amino)-1-oxopropyl)-1,2,3,4-tetrahydro-, (3s-(2(r*(r*)),3r*))-
quinaprilum [latin]
(3s)-2-{n-((s)-1-ethoxycarbonyl-3-phenylpropyl)-l-alanyl}-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
KBIO2_007213
KBIOGR_000994
KBIO3_002522
KBIO2_004645
KBIOSS_002077
KBIO2_002077
SPECTRUM2_000825
SPECTRUM4_000727
SPBIO_000749
SPECTRUM3_001551
NINDS_000710
IDI1_000710
BSPBIO_003022
NCGC00167962-01
NCGC00167962-02
HMS2090L05
HMS502D12
c09aa06
CHEMBL1592
(3s)-2-[(2s)-2-[[(2s)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]propanoyl]-3,4-dihydro-1h-isoquinoline-3-carboxylic acid
(3s)-2-[(2s)-2-[[(1s)-1-ethoxycarbonyl-3-phenyl-propyl]amino]propanoyl]-3,4-dihydro-1h-isoquinoline-3-carboxylic acid
A841331
NCGC00167962-03
quinapril [usp:inn:ban]
unii-rj84y44811
rj84y44811 ,
AKOS015950821
bdbm50368166
quinapril [mi]
quinapril [usp impurity]
quinapril [who-dd]
quinapril [inn]
quinapril [vandf]
gtpl6350
SCHEMBL15813
JSDRRTOADPPCHY-HSQYWUDLSA-N
AB00053714_08
AB00053714_09
DTXSID4023547 ,
(3s)-2-[(2s)-2-{[(2s)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}propanoyl]-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
3-isoquinolinecarboxylic acid, 2-[(2s)-2-[[(1s)-1-(ethoxycarbonyl)-3-phenylpropyl]amino]-1-oxopropyl]-1,2,3,4-tetrahydro-, (3s)-
SBI-0051931.P002
(s)-2-((s)-2-((s)-1-ethoxy-1-oxo-4-phenylbutan-2-ylamino)propanoyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
quinapril (korec)
Q596022
ci-906 (free acid)
BRD-K72222507-003-07-7
3-isoquinolinecarboxylic acid, 2-((2s)-2-(((1s)-1-(ethoxycarbonyl)-3-phenylpropyl)amino)-1-oxopropyl)-1,2,3,4-tetrahydro-, (3s)-
NCGC00167962-05
(3s)-2-((2s)-2-((1s)-1-ethoxycarbonyl-3-phenylpropylamino)propanoyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
(3s)-2-(n-((2s)-1-ethoxycarbonyl-4-phenylbutan-2-yl)-l-alanyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
(3s)-2-(n-((2s)-1-ethoxy-1-oxo-4-phenylbutan-2-yl)-l-alanyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
quinapril (usp impurity)
dtxcid303547

Research Excerpts

Overview

Quinapril is an angiotensin-converting enzyme inhibitor (ACE-inhibitor) and overdose can lead to prolonged hypotension. Quinapril has demonstrated anti-inflammatory properties in many disease states such as atherosclerosis, nephritis, scleroderma, diabetes and arthritis.

ExcerptReferenceRelevance
"Quinapril is a safe and well-tolerated antihypertensive medication with a favorable safety profile compared to other ACE inhibitors. "( Benefit and risk evaluation of quinapril hydrochloride.
Aronow, WS; Barkhordarian, M; Erbay, MI; Gupta, R; Lawrence, JA; Ulusan, S, 2023
)
2.64
"Quinapril is an effective drug for treatment of moderate ischemic heart failure."( [Angiotensin-converting enzyme, quinapril, in treating chronic cardiac failure].
Gadzhiev, AN, 2003
)
2.05
"Quinapril is an angiotensin-converting enzyme inhibitor (ACE-inhibitor) and overdose can lead to prolonged hypotension and, less frequently, transient renal impairment."( Auto-intoxication with flecainide and quinapril: ECG-changes, symptoms and treatment.
Dens, J; Van Reet, B, 2006
)
1.33
"Quinapril, which is a potent and selective inhibitor of both plasma and tissue ACE, has demonstrated anti-inflammatory properties in many disease states such as atherosclerosis, nephritis, scleroderma, diabetes and arthritis, and, thus, offers new therapeutic possibilities for disease treatment."( Anti-inflammatory actions of quinapril.
Egido, J; Ruiz-Ortega, M, 2007
)
2.07
"Only quinapril, which is a lipophilic ACE inhibitor with high affinity for tissue ACE, produced a significant improvement in flow-mediated brachial artery dilation in coronary artery disease patients; enalapril, losartan and amlodipine did not."( BANFF: an update.
Anderson, T, 1999
)
0.76
"Quinapril is an antihypertensive drug that belongs to the family of angiotensin-converting enzyme inhibitors. "( Solid-phase extraction and high-performance liquid chromatography applied to the determination of quinapril and its metabolite quinaprilat in urine.
Alonso, RM; Blanco, A; Jiménez, RM; Prieto, JA, 2001
)
1.97
"Quinapril is an antihypertensive drug commonly used in the treatment of hypertension and congestive heart failure. "( Determination of the angiotensin-converting enzyme inhibitor quinapril and its metabolite quinaprilat in pharmaceuticals and urine by capillary zone electrophoresis and solid-phase extraction.
Alonso, RM; Jiménez, RM; Prieto, JA, 2002
)
2
"Quinapril was shown to be a safe and effective treatment for patients with mild to moderate hypertension."( Quinapril versus atenolol in the treatment of mild to moderate essential hypertension.
Bahena, JH; Estrella, ME; Muñoz, M,
)
2.3
"Quinapril is a new ACE inhibitor that is converted to biologically active quinaprilat in the liver."( Adverse effects of angiotensin-converting enzyme inhibitors in antihypertensive therapy with focus on quinapril.
Materson, BJ, 1992
)
1.22
"Quinapril is a monoethyl ester which is hydrolysed after absorption to form an active metabolite, quinaprilat, which is a more potent angiotensin converting enzyme (ACE) inhibitor than the parent drug. "( Quinapril. A review of its pharmacological properties, and therapeutic efficacy in cardiovascular disorders.
Brogden, RN; Wadworth, AN, 1991
)
3.17
"Quinapril is a new non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor. "( Quinapril: a new second-generation ACE inhibitor.
Cetnarowski-Cropp, AB, 1991
)
3.17
"Quinapril is a new non-sulphydryl ACE inhibitor whose active metabolite, quinaprilat, has a relatively short accumulation half-life compared with enalapril and lisinopril but has an enhanced affinity for the converting enzyme, allowing rapid excretion of the drug while retaining a 24-hour antihypertensive effect with once-daily dosing."( ACE inhibitors in the treatment of hypertension in the older patient.
Canter, D; Frank, G, 1990
)
1
"Quinapril hydrochloride is a nonsulfhydryl angiotensin converting enzyme (ACE) inhibitor that has been extensively tested and found effective when administered once-a-day to hypertensive patients of both sexes and all degrees of hypertension and cardiac compromise, including those with left ventricular hypertrophy, with and without congestive heart failure. "( Use of quinapril in the elderly patient.
Schnaper, HW, 1990
)
2.18
"Quinapril is a recently introduced, nonsulfhydryl ACE inhibitor, whose intermediate half-life makes it well-suited for the treatment of patients with CHF."( Quinapril in chronic heart failure.
Dargie, HJ; Northridge, DB, 1990
)
2.44
"Quinapril is an orally active, non-peptide, nonsulfhydryl angiotensin-converting enzyme (ACE) inhibitor that acts potently and specifically to interrupt the conversion of angiotensin I to angiotensin II in both plasma and tissue. "( Quinapril--a preclinical review of the pharmacology, pharmacokinetics, and toxicology.
Andrews, LK; Kaplan, HR; Olson, SC; Taylor, DG, 1989
)
3.16
"Quinapril HCl is a novel, nonsulfhydryl angiotensin-converting enzyme (ACE) inhibitor. "( Quinapril: a double-blind, placebo-controlled trial in essential hypertension.
Maclean, D, 1989
)
3.16

Effects

Quinapril has an advantage over metoprolol succinate in therapy of patients with FC I-II CHF and preserved LF EF. Quinaprilat has a short elimination half-life but a potent binding affinity for ACE which enables once daily administration.

Quinapril has been extensively studied for efficacy and safety in patients with hypertension or congestive heart failure. Quinaprilat has a short elimination half-life (approximately 2 hours), but binds potently to and dissociates slowly from ACE.

ExcerptReferenceRelevance
"Quinapril has an advantage over metoprolol succinate in therapy of patients with FC I-II CHF and preserved LF EF at the background of stage I-II HD."( [Advantages of quinapril therapy in patients with arterial hypertension and functional class III chronic heart failure with preserved left ventricular ejection fraction].
Kanorskiĭ, SG; Pokrovskiĭ, VM; Tregubov, VG, 2012
)
2.17
"Quinaprilat has a short elimination half-life (approximately 2 hours), but binds potently to and dissociates slowly from ACE, thus allowing once or twice daily administration of quinapril in the treatment of patients with hypertension or congestive heart failure."( Quinapril. A reappraisal of its pharmacology and therapeutic efficacy in cardiovascular disorders.
Plosker, GL; Sorkin, EM, 1994
)
2.45
"Quinaprilat has a short elimination half-life but a potent binding affinity for ACE which enables once daily administration."( Quinapril. A review of its pharmacological properties, and therapeutic efficacy in cardiovascular disorders.
Brogden, RN; Wadworth, AN, 1991
)
2.45
"Quinaprilat has a strong binding capacity to tissue ACE allowing for once-daily dosing."( Quinapril: a new second-generation ACE inhibitor.
Cetnarowski-Cropp, AB, 1991
)
2.45
"Quinapril has similar to angiolin action directed effect to the connective tissue components, though losing as proteinconecting of hydroxiproline action."( [INFLUENCE OF QUINAPRIL IN COMBINATION WITH ANGIOLINE ON THE CONNECTIVE TISSUE COMPONENTS IN THE RATS SERUM WITH EXPERIMENTAL HYPERTENSION].
Belenichev, IF; Ghekman, IS; Gorchakova, NA; Kuzub, TA; Magomedov, S; Nagornaya, AA,
)
1.21
"Quinapril has an advantage over metoprolol succinate in therapy of patients with FC I-II CHF and preserved LF EF at the background of stage I-II HD."( [Advantages of quinapril therapy in patients with arterial hypertension and functional class III chronic heart failure with preserved left ventricular ejection fraction].
Kanorskiĭ, SG; Pokrovskiĭ, VM; Tregubov, VG, 2012
)
2.17
"Quinaprilat has a short elimination half-life (approximately 2 hours), but binds potently to and dissociates slowly from ACE, thus allowing once or twice daily administration of quinapril in the treatment of patients with hypertension or congestive heart failure."( Quinapril. A reappraisal of its pharmacology and therapeutic efficacy in cardiovascular disorders.
Plosker, GL; Sorkin, EM, 1994
)
2.45
"Quinapril has also been shown to reduce microalbuminuria in patients with hypertension and/or diabetes mellitus."( Quinapril: a further update of its pharmacology and therapeutic use in cardiovascular disorders.
Culy, CR; Jarvis, B, 2002
)
2.48
"Quinapril has been extensively studied for efficacy and safety in patients with hypertension or congestive heart failure (CHF) in the United States and Europe. "( Overview of quinapril, a new ACE inhibitor.
Frank, GJ; Knapp, LE; Olson, SC; Phelps, MC; Quade, MM; Rieger, MM; Sedman, AJ, 1990
)
2.1
"Quinaprilat has a short elimination half-life but a potent binding affinity for ACE which enables once daily administration."( Quinapril. A review of its pharmacological properties, and therapeutic efficacy in cardiovascular disorders.
Brogden, RN; Wadworth, AN, 1991
)
2.45
"Quinaprilat has a strong binding capacity to tissue ACE allowing for once-daily dosing."( Quinapril: a new second-generation ACE inhibitor.
Cetnarowski-Cropp, AB, 1991
)
2.45
"Quinapril has also been found to be the most potent of all available ACE inhibitors in binding to tissue ACE, which may contribute to its potent and sustained duration of action."( Overview of the clinical development of quinapril.
Frank, GJ, 1990
)
1.27
"Quinapril has the potential to affect plasma lipids beneficially or at least be "lipid neutral." Oral absorption of quinapril is rapid in rats, dogs, and monkeys."( Quinapril--a preclinical review of the pharmacology, pharmacokinetics, and toxicology.
Andrews, LK; Kaplan, HR; Olson, SC; Taylor, DG, 1989
)
2.44

Actions

Quinapril found to inhibit EPS, both macro- and microscopically, in a dose-dependent manner. Quinapril was used to inhibit ACE.

ExcerptReferenceRelevance
"Quinapril was found to inhibit EPS, both macro- and microscopically, in a dose-dependent manner."( An experimental model of encapsulating peritoneal sclerosis.
Fuchinoue, S; Ishii, Y; Kubota, K; Nakajima, I; Sawada, T; Teraoka, S, 2009
)
1.07
"Quinapril was used to inhibit ACE."( Neuromodulatory effects of the renin-angiotensin system on the cat electroretinogram.
Jacobi, PC; Jurklies, B; Osswald, H; Zrenner, E, 1994
)
1.01

Treatment

Quinapril-treated animals required less cardioversions for ventricular arrhythmias. Animals treated with 8 mg/kg q.d. had higher wall motion scores assessed by two-dimensional echocardiography.

ExcerptReferenceRelevance
"Quinapril treatment restored insulin-mediated microvascular recruitment and muscle glucose uptake in vivo."( A vascular mechanism for high-sodium-induced insulin resistance in rats.
Keske, MA; Premilovac, D; Rattigan, S; Richards, SM, 2014
)
1.12
"Quinapril-treated and amilodipine-treated rats displayed a lower glucose AUC than group C (P <.01), which had higher glucose levels than healthy controls (P <.001)."( Angiotension converting enzyme inhibition and calcium channel blockage improves cyclosporine induced glucose intolerance in rats.
Akalin, S; Akoğlu, E; Atakan, A; Koçak, H; Ozener, C; Tuğlular, S; Yavuz, DG,
)
0.85
"Quinapril treatment prevented the reduction of nephrin levels compared with the control group, while diltiazem treatment did not prevent the reduction. "( ACE inhibitors improve nephrin expression in Zucker rats with glomerulosclerosis.
Blanco, S; Bonet, J; Casas, I; López, D; Romero, R, 2005
)
1.77
"Quinapril treatment increased insulin-stimulated endothelial function in the type 2 diabetic subjects (P = 0.005), whereas forearm glucose uptake was unchanged. "( Quinapril treatment increases insulin-stimulated endothelial function and adiponectin gene expression in patients with type 2 diabetes.
Dominguez, H; Hansen, KW; Hawkins, M; Hermann, TS; Ihlemann, N; Kober, L; Li, W; Major-Pedersen, A; Nielsen, DB; Rask-Madsen, C; Torp-Pedersen, C, 2006
)
3.22
"Quinapril treatment increases insulin-stimulated endothelial function in patients with type 2 diabetes. "( Quinapril treatment increases insulin-stimulated endothelial function and adiponectin gene expression in patients with type 2 diabetes.
Dominguez, H; Hansen, KW; Hawkins, M; Hermann, TS; Ihlemann, N; Kober, L; Li, W; Major-Pedersen, A; Nielsen, DB; Rask-Madsen, C; Torp-Pedersen, C, 2006
)
3.22
"In quinapril-treated SHR compared with 36-week-old untreated SHR and age- and sex-matched Wistar-Kyoto (WKY) controls, we found 1) a lesser degree of LVH and a lesser level of blood pressure, 2) a lesser degree of interstitial fibrosis, represented by less interstitial collagen volume fraction (5.73 +/- 0.45% v 3.42 +/- 0.28%, P < .05; WKY, 3.44 +/- 0.66%), 3) a lower hydroxyproline concentration (1.09 +/- 0.05 mumol/L/g dry weight/100 g body weight to 0.81 +/- 0.05 mumol/L/g dry weight/100 g body weight, P < .05; WKY, 0.96 +/- 0.06 mumol/L/g dry weight/100 g body weight), 4) a lesser presence of collagen fibers, and 5) a lesser presence of collagen IV, fibronectin, and laminin.(ABSTRACT TRUNCATED AT 250 WORDS)"( Quinapril decreases myocardial accumulation of extracellular matrix components in spontaneously hypertensive rats.
Cenarruzabeitia, E; Díez, J; Galindo, MF; Hernández, M; Panizo, A; Pardo, J, 1995
)
2.25
"Quinapril treatment in elderly patients was efficacious and well tolerated, and quinapril appears to be an effective antihypertensive drug devoid of untoward effects on metabolic risk factors for cardiovascular disease."( Modification of cardiovascular risk factors during antihypertensive treatment: a multicentre trial with quinapril.
Capurso, A; Crepaldi, G; Manzato, E,
)
1.07
"quinapril treated)."( Preservation of left ventricular mechanical function and energy metabolism in rats after myocardial infarction by the angiotensin-converting enzyme inhibitor quinapril.
Ertl, G; Frantz, S; Gaudron, P; Horn, M; Hu, K; Hugel, S; Neubauer, S; Schnackerz, K, 1996
)
1.21
"Quinapril-treated SHR showed higher (P<.001) Bax expression than WKY and untreated SHR."( Is the regulation of apoptosis altered in smooth muscle cells of adult spontaneously hypertensive rats?
Díez, J; Hernández, M; Panizo, A; Pardo, J, 1997
)
1.02
"The quinapril treatment had no long-term blood pressure-lowering effect nor did it reduce the associated cardiac hypertrophy in deoxycorticosterone-NaCl hypertension."( Arterial function in mineralocorticoid-NaCl hypertension: influence of angiotensin-converting enzyme inhibition.
Hutri-Kähönen, N; Kähönen, M; Mäkynen, H; Pörsti, I; Tolvanen, JP; Wu, X, 1997
)
0.78
"In quinapril-treated SHR compared with untreated SHR, we found decreased expression of c-Myc (22% +/- 2%, P < .005) and cyclin A (13% +/- 1%, P < .001)."( Quinapril inhibits c-Myc expression and normalizes smooth muscle cell proliferation in spontaneously hypertensive rats.
Cenarruzabeitia, E; Díez, J; Galindo, MF; Hernández, M; Panizo, A; Pardo Mindán, FJ, 1997
)
2.25
"The quinapril treatment attenuated similarly both the LV/BW ratio and the ventricular AM levels."( Ventricular adrenomedullin levels correlate with the extent of cardiac hypertrophy in rats.
Dohi, K; Horio, T; Kangawa, K; Matsuo, H; Morimoto, A; Nagaya, N; Nishikimi, T; Yoshihara, F, 1999
)
0.78
"Quinapril treatment improved survival markedly (P<0.0000001) during the 24 weeks observation period."( Heart failure development in rats with ascending aortic constriction and angiotensin-converting enzyme inhibition.
Rupp, H; Turcani, M, 2000
)
1.03
"quinapril treatment results in an improvement of high-energy phosphate metabolism, of energy reserve via the creatine kinase reaction, and of contractile performance post-MI."( Preservation of cardiac function and energy reserve by the angiotensin-converting enzyme inhibitor quinapril during postmyocardial infarction remodeling in the rat.
Dienesch, C; Horn, M; Hügel, S; Neubauer, S; Remkes, H, 2001
)
1.97
"Quinapril treatment significantly prevented increases in both blood pressure and SSPG, with a return to the levels seen in the normal diet group."( Quinapril treatment restores the vasodilator action of insulin in fructose-hypertensive rats.
Hayakawa, T; Ito, T; Kamiya, H; Matsui, H; Nishimoto, Y; Okumura, K; Tomida, T; Uchida, T; Yamada, M,
)
2.3
"Quinapril-treated animals required less cardioversions for ventricular arrhythmias (1.58 +/- 0.40 vs 2.77 +/- 0.22; p < 0.05), had higher wall motion scores assessed by two-dimensional echocardiography (4 = normal to -1 = dyskinesia; 2.11 +/- 0.10 vs 1.50 +/- 0.07; p < 0.05), more complete coronary artery endothelial relaxation to bradykinin (45% +/- 3% vs 7% +/- 4%; p < 0.005), and lower infarct size (24.0% +/- 3.0% vs 40.0% +/- 1.7%; p < 0.0001)."( Pretreatment with angiotensin-converting enzyme inhibitors attenuates ischemia-reperfusion injury.
Bao, Y; Bernard, SA; Lazar, HL; Rivers, S, 2002
)
1.76
"quinapril, and six dogs treated with 8 mg/kg q.d."( Quinapril, an angiotensin converting enzyme inhibitor, prevents cardiac hypertrophy during episodic hypertension.
Brant, D; Julius, S; Krause, L; Li, Y; Taylor, D, 1991
)
2.45
"Only treatment with quinapril was associated with improvement of RAS, elevation of tolerance to physical effort, and increased VO2max."( [Advantages of quinapril therapy in patients with arterial hypertension and functional class III chronic heart failure with preserved left ventricular ejection fraction].
Kanorskiĭ, SG; Pokrovskiĭ, VM; Tregubov, VG, 2012
)
1.05
"Treatment with quinapril significantly lowered systolic blood pressure and ventricular weight in both SHR and WKY."( Quinapril effects on resistance artery structure and function in hypertension.
Gao, YJ; Lee, RM; Yang, L, 2004
)
2.11
"Treatment with quinapril and atorvastatin reduced ventricular weight in SHR and normalized the augmented contractile responses to norepinephrine but did not alter the contraction to electric field stimulation."( The effects of quinapril and atorvastatin on artery structure and function in adult spontaneously hypertensive rats.
Gao, YJ; Lee, RM; Yang, L, 2005
)
1.02
"Treatment with quinapril or losartan decreased caspase-3 activation, 4-hydroxy-2-nonenal staining, and 8-iso-PGF2alpha levels and increased Cu/Zn superoxide dismutase expression."( Long-term blood pressure control prevents oxidative renal injury.
Egido, J; Esteban, V; Gallego-Delgado, J; Justo, P; Lazaro, A; Mezzano, S; Ortiz, A; Osende, J,
)
0.47
"4. Treatment with quinapril was associated with a significant rise in plasma renin activity (PRA) of 8.83 ng AI ml-1 h-1 (95% C.I."( Haemodynamic response and pharmacokinetics after the first dose of quinapril in patients with congestive heart failure.
Hillis, WS; Lees, KR; Macfadyen, RJ; Reid, JL; Squire, IB, 1994
)
0.85
"Posttreatment with quinapril also reversed the glomerular injury (subcapsular, -83%; juxtamedullary, -56%) and arteriolar (-87%) injury scores obtained from renal biopsy specimens (P < .005 and P < .0001, respectively)."( ACE inhibition prevents and reverses L-NAME-exacerbated nephrosclerosis in spontaneously hypertensive rats.
Frohlich, ED; Ono, H; Ono, Y, 1996
)
0.61
"Treatment with quinapril was also accompanied by normalization in the myocardial structure of the right ventricles of SHR."( Are mast cells involved in hypertensive heart disease?
Cenarruzabeitia, E; Díez, J; Galindo, MF; Hernández, M; Mindán, FJ; Panizo, A, 1995
)
0.63
"Treatment with quinapril for 6 months appears to have advantages over metoprolol in NIDDM patients with hypertension. "( Comparison of effects of quinapril and metoprolol on glycaemic control, serum lipids, blood pressure, albuminuria and quality of life in non-insulin-dependent diabetes mellitus patients with hypertension. Swedish Quinapril Group.
Asplund, K; Bystedt, T; Dahlöf, B; Jern, S; Kjellström, T; Lithell, H; Ostman, J, 1998
)
0.96
"Treatment with quinapril, but not with losartan, was associated with a decrease in both PAI-1 antigen (P=0.03) and activity (P=0.018)."( Comparative effect of angiotensin-converting enzyme inhibition and angiotensin II type 1 receptor antagonism on plasma fibrinolytic balance in humans.
Agirbasli, M; Brown, NJ; Vaughan, DE, 1999
)
0.64
"Treatment with quinapril significantly reduced clinical ischemic events after CABG: 15% in patients on placebo versus 4% of patients on quinapril (hazard ratio 0.23, 95% confidence interval 0.06 to 0.87, p = 0.02)."( Effects of quinapril on clinical outcome after coronary artery bypass grafting (The QUO VADIS Study). QUinapril on Vascular Ace and Determinants of Ischemia.
Buikema, H; Crijns, HJ; Grandjean, JG; Kingma, JH; Oosterga, M; Pinto, YM; van Gilst, WH; Voors, AA, 2001
)
1.04

Toxicity

The results of more than 1600 patient years of experience with the new angiotensin converting enzyme (ACE) inhibitor, quinapril, suggest that it is safe for the treatment of hypertension and congestive heart failure. Quinapril was well tolerated in all trials, with the incidence of adverse events and withdrawals tending to be lower with quinabril than with enalapril or captopril.

ExcerptReferenceRelevance
" Adverse reactions to this drug class are rarely serious."( Adverse effects of angiotensin-converting enzyme inhibitors in antihypertensive therapy with focus on quinapril.
Materson, BJ, 1992
)
0.5
" A comparison of the double-blind studies demonstrated that quinapril has a lower incidence of adverse events and/or withdrawals than reported for captopril or enalapril."( The safety and tolerability of quinapril.
Frank, GJ; Knapp, LE; McLain, R; Posvar, E; Rieger, MM; Singer, R, 1990
)
0.81
" Quinapril was well tolerated in all trials, with the incidence of adverse events and withdrawals tending to be lower with quinapril than with enalapril or captopril."( The safety and efficacy of quinapril in the treatment of mild to moderate essential hypertension.
Frishman, WH, 1990
)
1.49
" A comparison of double-blind studies showed quinapril to have a lower incidence of adverse effects and withdrawals than reported for captopril or enalapril."( The safety profile of quinapril: is there a difference among ACE inhibitors?
Canter, D; Frank, GJ; Knapp, LE; McLain, RW, 1990
)
0.85
"The results of more than 1600 patient years of experience with the new angiotensin converting enzyme (ACE) inhibitor, quinapril, suggest that it is safe for the treatment of hypertension and congestive heart failure."( Does the duration of action of angiotensin converting enzyme inhibitors affect their safety and adverse effects?
Frank, GJ, 1989
)
0.49
"A comprehensive analysis of the reporting of adverse events, withdrawals due to adverse events, and serious adverse events has been conducted on 2,010 patients treated with quinapril hydrochloride."( Overall tolerance and safety of quinapril in clinical trials.
Frank, GJ; Knapp, LE; McLain, RW, 1989
)
0.75
" This approach does not necessarily detect the rare adverse events that may only be observed when very large numbers of patients are studied."( Analysis of adverse effects among patients with essential hypertension receiving an ACE inhibitor or a beta-blocker.
Bahrmann, H; Baumgart, P; Benkert, K; Bönner, G; Frohlich, ED; Klein, G; Neiss, A; Rosenthal, J; Schnelle, K,
)
0.13
"Antihypertensive medication doses are typically increased within several weeks after initiation of therapy because of inadequate blood pressure (BP) control and/or adverse effects."( The rapidity of drug dose escalation influences blood pressure response and adverse effects burden in patients with hypertension: the Quinapril Titration Interval Management Evaluation (ATIME) Study. ATIME Research Group.
Flack, JM; Holmes, CB; McLean, B; Mensah, G; Preisser, J; Saunders, E; Yunis, C, 2000
)
0.51
"7% of participants experienced adverse events vs 10."( The rapidity of drug dose escalation influences blood pressure response and adverse effects burden in patients with hypertension: the Quinapril Titration Interval Management Evaluation (ATIME) Study. ATIME Research Group.
Flack, JM; Holmes, CB; McLean, B; Mensah, G; Preisser, J; Saunders, E; Yunis, C, 2000
)
0.51
"Slower dose escalation of the angiotensin-converting enzyme inhibitor quinapril provides higher BP control rates and fewer serious adverse events than more rapid drug dose escalation."( The rapidity of drug dose escalation influences blood pressure response and adverse effects burden in patients with hypertension: the Quinapril Titration Interval Management Evaluation (ATIME) Study. ATIME Research Group.
Flack, JM; Holmes, CB; McLean, B; Mensah, G; Preisser, J; Saunders, E; Yunis, C, 2000
)
0.74
" In another instance heart block and hypotension was noted in association with a diltiazem and atenolol adverse interaction."( Aminophylline reversal of antihypertensive agent toxicity.
Roberge, RJ; Rosetti, JM; Rossetti, ML, 2001
)
0.31
"Presented is an unusual case of a 66-year-old-resident of a long-term care facility, who manifested severe dysgeusia and impaired quality of life attributed to the angiotensin-converting enzyme (ACE) inhibitor enalapril; not realized at the time was the fact that he had an adverse reaction-cough-just weeks earlier from another ACE inhibitor in the same class, quinapril, thus illustrating different adverse effects to two antihypertensives in the same class."( If it is not cough, it must be dysgeusia: differing adverse effects of angiotensin-converting enzyme inhibitors in the same individual.
Dharmarajan, TS; Murakonda, P; Unnikrishnan, D,
)
0.3
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36

Pharmacokinetics

This review compares the metabolism and pharmacokinetic profiles of captopril, the first orally active angiotensin-converting enzyme (ACE) inhibitor, and 2 newer ACE inhibitors, enalapril and quinapril. The Pharmacokinetic profile of quinil in these CAPD patients was not significantly different from that previously observed in healthy subjects with normal renal function.

ExcerptReferenceRelevance
" Quinaprilat was detectable in plasma up to 72 hours after all doses and the terminal phase half-life was calculated at 26 +/- 7 hours."( Dose responses and pharmacokinetics for the angiotensin converting enzyme inhibitor quinapril.
Elliott, HL; Macdonald, NJ; Meredith, PA; Reid, JL, 1992
)
1.42
"This review compares the metabolism and pharmacokinetic profiles of captopril, the first orally active angiotensin-converting enzyme (ACE) inhibitor, and 2 newer ACE inhibitors, enalapril and quinapril."( Comparative pharmacokinetics of captopril, enalapril, and quinapril.
Haynie, R; Vertes, V, 1992
)
0.72
" In contrast, quinaprilat maximum plasma concentration, trough and peak steady-state plasma concentrations, area under the plasma concentration-time curve, and half-life increased significantly with increasing renal insufficiency."( The pharmacokinetics of quinapril and its active metabolite, quinaprilat, in patients with various degrees of renal function.
Abraham, PA; Halstenson, CE; Horvath, AM; Olson, SC; Opsahl, JA; Posvar, EL; Rachael, K, 1992
)
0.95
" The pharmacokinetic profile of quinapril in these CAPD patients was not significantly different from that previously observed in healthy subjects with normal renal function and in patients with moderate to severe renal dysfunction not yet requiring dialysis (RDND)."( Pharmacokinetics of quinapril and its active metabolite quinaprilat during continuous ambulatory peritoneal dialysis.
Horvath, AM; Olson, SC; Posvar, EL; Starmann, B; Swartz, RD, 1990
)
0.89
" Comparable mean quinapril pharmacokinetic parameter values as well as comparable mean quinaprilat pharmacokinetic parameter values determined following quinapril administered alone and following quinapril administered with propranolol, indicate that propranolol does not alter the single dose pharmacokinetics of quinapril or quinaprilat."( Multiple-dose propranolol administration does not influence the single dose pharmacokinetics of quinapril and its active metabolite (quinaprilat).
Caillé, G; Colburn, WA; Ferry, JJ; Frank, GJ; Horvath, AM; Lacasse, Y; Olson, SC; Pilon, D, 1990
)
0.84
" From these pharmacokinetic and pharmacodynamic properties, it follows that the dose rate of the ACE inhibitors should be reduced in direct proportion to the degree of reduction in renal function."( The pharmacokinetics of angiotensin converting enzyme inhibitors in patients with renal impairment.
Bailey, RR; Begg, EJ; Frank, GJ; Lynn, KL; Olson, SC; Robson, RA, 1989
)
0.28
" Peak plasma concentrations of these metabolites are similar to that of Q, and each is eliminated rapidly with a half-life of approximately one hour."( The clinical pharmacokinetics of quinapril.
Colburn, WA; Horvath, AM; Michniewicz, BM; Olson, SC; Sedman, AJ; Welling, PG, 1989
)
0.56
"The potential effect of cimetidine on the pharmacokinetic profiles of quinapril and its active metabolite CI-928 was evaluated in eight healthy volunteers."( Multiple-dose cimetidine administration does not influence the single-dose pharmacokinetics of quinapril and its active metabolite (CI-928).
Cetnarowski, AB; Ferry, JJ; Horvath, AM; Sedman, AJ; Thomas, RW, 1988
)
0.73
"5 hour in quinapril and CI-928 tmax values were observed after consumption of food."( Influence of food on the pharmacokinetics of quinapril and its active diacid metabolite, CI-928.
Colburn, WA; Ferry, JJ; Horvath, AM; Latts, JR; Sedman, AJ,
)
0.79
" The pharmacokinetic profiles of quinapril and the active metabolite quinaprilat were determined."( Haemodynamic response and pharmacokinetics after the first dose of quinapril in patients with congestive heart failure.
Hillis, WS; Lees, KR; Macfadyen, RJ; Reid, JL; Squire, IB, 1994
)
0.81
" Increases in the apparent elimination half-life and in AUC(0, 12h) values of quinaprilat were associated with smaller ejection fractions, decreased creatinine clearance, and increased patient age."( The pharmacokinetics of quinapril and quinaprilat in patients with congestive heart failure.
Bammert-Adams, JA; Begg, EJ; Ikram, H; Olson, SC; Posvar, EL; Reece, PA; Richards, AM; Robson, RA; Sedman, AJ, 1994
)
0.82
" Pharmacodynamic effects of quinaprilat and oral quinapril were assessed by measurement of blood pressure changes after an infusion of angiotensin I (A-I) at a dose previously determined to produce an increase in diastolic blood pressure of 25 mmHg under standardized conditions (A-I pressor response)."( A pharmacodynamic and pharmacokinetic comparison of intravenous quinaprilat and oral quinapril.
Breslin, E; Jahnchen, E; Neub, M; Posvar, E; Trenk, D, 1996
)
0.83
"The pharmacokinetic interaction between cefdinir and an angiotensin-converting enzyme inhibitor (captopril or quinapril) was investigated in rats."( Pharmacokinetic interaction between cefdinir and two angiotensin-converting enzyme inhibitors in rats.
Jacolot, A; Petitjean, O; Tod, M, 1996
)
0.51
"Oligopeptidic drugs such as beta-lactams and angiotensin-converting enzyme inhibitors share the same carriers in humans and animals, which results in possible pharmacokinetic interactions."( Analysis of the pharmacokinetic interaction between cephalexin and quinapril by a nonlinear mixed-effect model.
Padoin, C; Perret, G; Petitjean, O; Tod, M, 1998
)
0.54
" The pharmacokinetic parameters were analyzed by noncompartmental analysis and the ANOVA was carried out using logarithmically transformed data of the AUC and C as well as untransformed T(max)."( Pharmacokinetics and bioequivalence study of the two 20-mg quinapril hydrochloride tablet formulations in healthy Thai male volunteers.
Jengjareon, A; Kumsorn, B; Nasangiam, N; Rojanasthien, N; Roongapinun, S, 2008
)
0.59
" The half-life of quinapril (1."( Pharmacokinetics and bioequivalence study of the two 20-mg quinapril hydrochloride tablet formulations in healthy Thai male volunteers.
Jengjareon, A; Kumsorn, B; Nasangiam, N; Rojanasthien, N; Roongapinun, S, 2008
)
0.92
" Noncompartmental pharmacokinetic modelling and statistical analyses were performed."( Effects of quinapril on angiotensin converting enzyme and plasma renin activity as well as pharmacokinetic parameters of quinapril and its active metabolite, quinaprilat, after intravenous and oral administration to mature horses.
Barlow, BM; Breuhaus, BA; Davis, JL; Kruger, K; LaFevers, DH; Schirmer, JM, 2014
)
0.79
" The CES1 genotype had no significant effect on the enalaprilat to enalapril AUC0-∞ ratio or on any other pharmacokinetic or pharmacodynamic parameters of enalapril or enalaprilat."( Effect of carboxylesterase 1 c.428G > A single nucleotide variation on the pharmacokinetics of quinapril and enalapril.
Backman, JT; Holmberg, MT; Launiainen, T; Neuvonen, PJ; Niemi, M; Tarkiainen, EK; Tornio, A, 2015
)
0.64

Compound-Compound Interactions

Study was aimed at assessing the effects of losartan or its combination with quinapril on the cardiac nervous system and neurohormonal status in essential hypertension. Forty patients with moderate to severe hypertension and daytime ambulatory diastolic blood pressure > or = 90 mm Hg were randomized double-blind to treatment. This observation revealed a possible transporter-mediated drug-drug interaction (DDI) between gemcabene and quInapril.

ExcerptReferenceRelevance
" Forty patients with moderate to severe hypertension and daytime ambulatory diastolic blood pressure > or = 90 mm Hg were randomized double-blind to once-daily treatment with either quinapril up to 20 mg (n = 20) or atenolol up to 100 mg (n = 20) as single drugs or in combination with hydrochlorothiazide 25 mg over a period of 12 weeks."( Comparison of quinapril and atenolol as single drugs or in combination with hydrochlorothiazide in moderate to severe hypertensives, using automated ambulatory monitoring.
Lacourcière, Y; Lefebvre, J; Poirier, L; Provencher, P, 1993
)
0.84
" This study was aimed at assessing the effects of losartan or its combination with quinapril on the cardiac nervous system and neurohormonal status in essential hypertension."( Effects of losartan and its combination with quinapril on the cardiac sympathetic nervous system and neurohormonal status in essential hypertension.
Doi, O; Ishikawa, J; Nawada, R; Obayashi, K; Sakata, K; Tamekiyo, H; Yoshida, H, 2002
)
0.8
" This observation revealed a possible transporter-mediated drug-drug interaction (DDI) between gemcabene and quinapril."( Renal organic anion transporter-mediated drug-drug interaction between gemcabene and quinapril.
Bond, BR; Chupka, J; Feng, B; Heath, TG; Yu, Y; Yuan, H; Zheng, JY, 2009
)
0.79

Bioavailability

Quinapril following oral administration was <5%. intravenous quinapilat should produce a pharmacodynamic response similar to that obtained with oral quinAPril at approximately half the dose. The mean absorption rate constant of cephalexin was significantly lowered by quinabril (from 0.3 to 0.2%)

ExcerptReferenceRelevance
" Based on the concentrations of quinaprilat observed in this study, the absolute bioavailability of quinapril was approximately 50%; intravenous quinaprilat should therefore produce a pharmacodynamic response similar to that obtained with oral quinapril at approximately half the dose."( A pharmacodynamic and pharmacokinetic comparison of intravenous quinaprilat and oral quinapril.
Breslin, E; Jahnchen, E; Neub, M; Posvar, E; Trenk, D, 1996
)
0.82
" We suggest that ADMA activates the local renin-angiotensin system, and the angiotensin II released activates NAD(P)H oxidase; superoxide produced interferes with the bioavailability of NO, resulting in diminished flow-induced dilation, a mechanism that may contribute to the development of arteriolar dysfunction and increased tone associated with elevated ADMA levels."( ADMA impairs nitric oxide-mediated arteriolar function due to increased superoxide production by angiotensin II-NAD(P)H oxidase pathway.
Koller, A; Lotz, G; Racz, A; Veresh, Z, 2008
)
0.35
"Angiotensin-converting enzyme (ACE) inhibitors differ in their lipophilic/hydrophilic index that determines their tissue bioavailability and affinity to ACE, which may result in major differences in the degree of blockade of cardiac ACE."( Effects of ACE inhibitors on cardiac angiotensin II and aldosterone in humans: "Relevance of lipophilicity and affinity for ACE".
Coletta, E; Davies, R; Haddad, H; Leenen, FH; Ruzicka, M; White, R, 2010
)
0.36
" Nebivolol could have a better impact than atenolol on arterial stiffness, by increasing the bioavailability of endothelium-derived nitric oxide."( Effects of renin-angiotensin-aldosterone system inhibitors and beta-blockers on markers of arterial stiffness.
Athyros, VG; Karagiannis, A; Katsiki, N; Koumaras, C; Mikhailidis, DP; Stavrinou, E; Tziomalos, K, 2014
)
0.4
" Bioavailability of quinapril following oral administration was <5%."( Effects of quinapril on angiotensin converting enzyme and plasma renin activity as well as pharmacokinetic parameters of quinapril and its active metabolite, quinaprilat, after intravenous and oral administration to mature horses.
Barlow, BM; Breuhaus, BA; Davis, JL; Kruger, K; LaFevers, DH; Schirmer, JM, 2014
)
1.12

Dosage Studied

After the double-blind trial, 189 patients entered a 1-year, open-label study. Male rats were dosed orally with quinapril at 0 (vehicle control) or 400 mg/kg for 1, 3, 8, 17 or 29 days. High plasma concentrations of gemcabene (>100 microM) achieved in humans and rats upon oral dosing.

ExcerptRelevanceReference
" Although blood pressures were measured by the patients using sphygmomanometers of the same type and the physicians, decisions to treat or to increase dosage were based on the patients' recordings only."( [Comparison of results of daily blood pressure self-monitoring and general practice monitoring within the scope of a study assessing treatment of hypertension with quinapril].
Deischler, H; Fiedler, L; Harpf, H; Havelec, L; Kindermann, T; Magometschnigg, D; Neumüller, M; Pap, S; Schnögl, H; Spitzer, D, 1992
)
0.48
"5 mg to produce any further increase in the magnitude of ACE inhibition is consistent with an maximum effect dose-response relationship, with the obvious implication that higher doses will increase only the duration not the magnitude of response."( Dose responses and pharmacokinetics for the angiotensin converting enzyme inhibitor quinapril.
Elliott, HL; Macdonald, NJ; Meredith, PA; Reid, JL, 1992
)
0.51
" The patients were studied without any pretreatment (n = 14) or after 1 week of treatment with the oral ACE inhibitor quinapril at a dosage of 10 mg/day (n = 11)."( Angiotensin converting enzyme inhibition restores cardiac and hormonal responses to volume overload in patients with dilated cardiomyopathy and mild heart failure.
deCampora, P; DeLuca, N; Enea, I; Lembo, G; Mele, AF; Rendina, V; Romano, M; Rubattu, S; Tritto, C; Volpe, M, 1992
)
0.49
" Thus, quinapril dosage adjustment may be required in some patients with renal impairment."( The pharmacokinetics of quinapril and its active metabolite, quinaprilat, in patients with various degrees of renal function.
Abraham, PA; Halstenson, CE; Horvath, AM; Olson, SC; Opsahl, JA; Posvar, EL; Rachael, K, 1992
)
1.05
" Three hemodynamic trials, two of which included both acute and long-term phases, and one placebo-controlled, dose-response study have been conducted in 333 patients with CHF."( Overview of quinapril, a new ACE inhibitor.
Frank, GJ; Knapp, LE; Olson, SC; Phelps, MC; Quade, MM; Rieger, MM; Sedman, AJ, 1990
)
0.66
" The usual effective dosage of quinapril was 10-40 mg/day, with some patients receiving up to 80 mg/day."( The treatment of mild to moderate hypertension with ACE inhibitors.
Taylor, SH, 1990
)
0.57
" Plasma and kidney tissues showed increasing ACE inhibition in a dose-dependent manner after oral dosing with quinapril."( Inhibition of angiotensin-converting enzyme (ACE) in plasma and tissue.
Chen, BZ; Fabris, B; Johnston, CI; Perich, R; Pupic, V, 1990
)
0.49
" The former features are of particular use in evaluating the duration of action and dose-response relationships for new antihypertensive drugs, especially those developed for once daily dosing."( The contribution of ambulatory blood pressure measurement to the evaluation of new antihypertensive drugs.
Bainbridge, AD; MacFadyen, RJ; Reid, JL, 1991
)
0.28
" These results suggest that the dosage rate of quinapril may have to be altered in renal impairment."( The pharmacokinetics and pharmacodynamics of quinapril and quinaprilat in renal impairment.
Bailey, RR; Begg, EJ; Frank, GJ; Lynn, KL; Olson, SC; Robson, RA, 1990
)
0.8
" Results of these studies supported the recommendation of a once daily dosage of quinapril, 10-40 mg, as first-line therapy in the management of hypertension, with diuretics as concomitant therapy as required in patients with severe hypertension."( Overview of the clinical development of quinapril.
Frank, GJ, 1990
)
0.77
" Blood pressure reduction was observed in four of six patients, with onset reliably two to four hours after dosing and duration up to 48 hours, associated with quinaprilat concentrations in plasma above 90 ng/mL for at least 33 hours postdose."( Pharmacokinetics of quinapril and its active metabolite quinaprilat during continuous ambulatory peritoneal dialysis.
Horvath, AM; Olson, SC; Posvar, EL; Starmann, B; Swartz, RD, 1990
)
0.8
" During a 12 week, double-blind phase, the dosage of quinapril was increased from 10 to 40 mg twice daily being doubled every 4 weeks."( Effects of the converting enzyme inhibitor quinapril (CI-906) on blood pressure, renin-angiotensin system, and prostanoids in essential hypertension.
Manninen, V; Nurmi, AK; Pörsti, I; Pörsti, P; Säynävälammi, P; Seppälä, E; Vapaatalo, H, 1988
)
0.79
" Reductions in DBP of up to 13 mm Hg were obtained, and in full dosage more than 65% of patients achieved a reduction in DBP of 10 mm Hg or more from baseline or reduced their DBP to 90 mm Hg or less."( Quinapril: a double-blind, placebo-controlled trial in essential hypertension.
Maclean, D, 1989
)
1.72
" Nineteen evaluable patients who had responded to acute therapy received an additional sixteen weeks of chronic treatment with quinapril in individualized dosage regimens."( Preliminary hemodynamic report of the efficacy and safety of quinapril in acute and chronic treatment of patients with congestive heart failure.
Banas, JS, 1989
)
0.72
" Patients with MRI initially received quinapril 5 mg once daily (qd) followed by titration to a maximum dosage of 40 mg/day (furosemide optional at 40 mg only)."( Quinapril hydrochloride effects on renal function in patients with renal dysfunction and hypertension: a drug-withdrawal study.
Canter, D; Gmerek, A; Miller, MA; Robbins, J; Shurzinske, L; Texter, M, 1994
)
2
"A factorial design method was applied in this multicentre trial of the angiotensin-converting enzyme inhibitor quinapril hydrochloride (Accupril) in combination with the diuretic hydrochlorothiazide (HCTZ) to assess the additive effects of the combination versus monotherapy, to characterise the dose-response relationship of each drug in the presence of the other and to determine if quinapril would attenuate the hypokalemic effect of HCTZ."( Quinapril and hydrochlorothiazide combination for control of hypertension: assessment by factorial design. Quinapril Investigator Group.
Canter, D; Frank, GJ; Knapp, LE; Phelps, M; Quade, M; Texter, M, 1994
)
1.94
" Quinapril doses were titrated upward at 4-week intervals to three dosage levels."( Quinapril in the treatment of hypertension in primary care centers.
Alcocer, L; Novoa, G; Sotres, D,
)
2.48
" Dosing of quinapril in patients with CHF should be based on their renal function."( The pharmacokinetics of quinapril and quinaprilat in patients with congestive heart failure.
Bammert-Adams, JA; Begg, EJ; Ikram, H; Olson, SC; Posvar, EL; Reece, PA; Richards, AM; Robson, RA; Sedman, AJ, 1994
)
0.99
" Male rats were dosed orally with quinapril at 0 (vehicle control) or 400 mg/kg for 1, 3, 8, 17 or 29 days."( Effects of the angiotensin-converting enzyme inhibitor quinapril on renal function in rats.
Dethloff, LA; Graziano, MJ; Griffin, HE; Pegg, DG,
)
0.66
") dosing was compared with twice daily (b."( A multicentre, double-blind, placebo-controlled trial of quinapril in mild, chronic heart failure.
Dargie, HJ; Elder, AT; Henderson, E; Lahiri, A; Northridge, DB; Raftery, ED; Rose, E; Shaw, TR, 1993
)
0.53
" Differences exist between the dosage schedules of both ACE inhibitors."( [Treatment of heart failure in dogs with ACe inhibitors: comparison of quinapril and captopril].
Kersten, U; Morisse, B, 1995
)
0.52
" Antihypertensive therapy has been traditionally dosed in the morning after awakening, and in recent years most of the newly developed antihypertensive agents have been once-daily, long-acting preparations."( A chronotherapeutic approach to the management of hypertension.
White, WB, 1996
)
0.29
" The dose-response and duration-of-effect after single intravenous doses of quinaprilat and placebo (part A) and after administration of oral quinapril solution and intravenous quinaprilat (part B) were assessed in a randomized, crossover study of two groups of 12 healthy volunteers."( A pharmacodynamic and pharmacokinetic comparison of intravenous quinaprilat and oral quinapril.
Breslin, E; Jahnchen, E; Neub, M; Posvar, E; Trenk, D, 1996
)
0.76
" This parameter may provide a useful index for ACE inhibitor dosage adjustment during chronic therapy."( Acute and long-term dose-response study of quinapril on hormonal profile and tissue angiotensin-converting enzyme in Wistar rats.
Baudin, B; Bernard, M; Carayon, A; Ciferri, S; Fernando Ramirez-Gil, J; Lechat, P; Mougenot, N; Schaison, FH, 1996
)
0.56
" Further, the urinary recovery of quinapril and quinaprilat (after dosing quinapril into proximal segments) was urine flow rate dependent."( Reabsorption and metabolism of quinapril and quinaprilat in rat kidney: in vivo micropuncture studies.
Kugler, AR; Schnermann, JB; Smith, DE, 1995
)
0.86
" For nonresponders, the dosage was titrated up to a maximum of 40 mg."( Usefulness of low-dose, once-daily quinapril as monotherapy for patients with hypertension.
Alcocer, L; Novoa, G; Olvera, S,
)
0.41
" Acute toxicity is minimal in rodents, and repeated dosing elicits gastric irritation, juxtaglomerular apparatus (JGA) hypertrophy and hyperplasia and tubular degenerative changes in the kidney, and reduced red cell parameters and heart weights in rodents and/or dogs."( Preclinical toxicology studies with the angiotensin-converting enzyme inhibitor quinapril hydrochloride (Accupril).
Anderson, JA; de la Iglesia, FA; Gough, AW; Herman, JR; McGuire, EJ; Pegg, DG; Theiss, JC, 1996
)
0.52
"Antihypertensive drug combinations have two major advantages: First, dosage of the single components can be reduced, and second, putative side effects can be minimized."( [Combination antihypertensive therapy in patients with an increased risk profile].
Bartens, W; Nauck, M; Wanner, C, 1996
)
0.29
" Thereafter, the dosage was adjusted according to the response of blood pressure to a desired value (BP < 140/90 mmHg)."( Effect of quinapril therapy on blood pressure and serotonin change in patients with mild to moderate hypertension.
Chen, YT; Cheng, FC; Huang, JL; Ting, CT, 1996
)
0.7
" Two patients treated with quinaprilat withdrew due to hypotension; one patient required a dosage reduction."( Assessing the clinical need for short-term conversion from oral to parenteral angiotensin converting enzyme inhibitor therapy in hypertensive patients. A quinapril to quinaprilat placebo-controlled model.
Canter, D; Goldstein, R; McCormick, L; Whelton, A; Wombolt, D, 1997
)
0.79
"Although angiotensin-converting enzyme inhibitors are beneficial for patients with congestive heart failure, the appropriate timing and dosage in acute myocardial infarction are still controversial."( Cardioprotective effects of quinapril after myocardial infarction in hypertensive rats.
Kawamura, K; Kubota, J; Mori, T; Nishimura, H; Okabe, M; Ueyama, M, 1998
)
0.59
" The dose-response curves of vasoconstriction to phenylephrine and prostaglandin F2alpha were obtained in healthy male volunteers."( Attenuation by ACE inhibitor drugs of alpha-adrenoceptor sensitivity in human vessels: possible differences related to drug lipophilicity.
Kimura, M; Kosuge, K; Nakashima, M; Nishimoto, M; Ohashi, K; Umemura, K, 1998
)
0.3
"The ACEIs shifted the dose-response curve of phenylephrine to the right and raised the median effective dose (ED50; 189."( Attenuation by ACE inhibitor drugs of alpha-adrenoceptor sensitivity in human vessels: possible differences related to drug lipophilicity.
Kimura, M; Kosuge, K; Nakashima, M; Nishimoto, M; Ohashi, K; Umemura, K, 1998
)
0.3
" Four days before necropsy, mice were dosed with bromodeoxyuridine (BrdU) using osmotic pumps."( Troglitazone-induced heart and adipose tissue cell proliferation in mice.
Breider, MA; de la Iglesia, FA; Gough, AW; Haskins, JR; Sobocinski, G,
)
0.13
" Pretreatment with 10 mg of quinapril significantly shifted the dose-response curve for bradykinin to the left (effect of quinapril; F = 77."( Inhibition of aminopeptidase P potentiates wheal response to bradykinin in angiotensin-converting enzyme inhibitor-treated humans.
Brown, NJ; Kim, KS; Kumar, S; Simmons, WH, 2000
)
0.6
" The ET-1 dose-response was biphasic in normal muscles."( Myocardial contractile responsiveness to endothelin-1 in the post-infarction rat model of heart failure: effects of chronic quinapril.
Cernacek, P; Nguyen, QT; Picard, P; Qi, XL; Rouleau, JL; Sia, YT; Sirois, M; Stewart, DJ; Wei, G, 2001
)
0.52
" However, a lower dosage of quinapril (20 mg/day) showed no effect on ischaemic events or atherosclerotic progression with 3 years of treatment in a similarly designed study involving 1750 patients undergoing coronary angioplasty."( Quinapril: a further update of its pharmacology and therapeutic use in cardiovascular disorders.
Culy, CR; Jarvis, B, 2002
)
2.05
" Quinapril 40 mg/day also significantly reduced the incidence of ischaemic events in patients undergoing CABG in one study; however, a lower dosage of quinapril (20 mg/day) had no effect on ischaemic events in patients undergoing coronary angioplasty in another trial."( Quinapril: a further update of its pharmacology and therapeutic use in cardiovascular disorders.
Culy, CR; Jarvis, B, 2002
)
2.67
" Dosing on a mg/kg basis resulted in quinaprilat AUC and Cmax values that were generally comparable across the age range of patients in this study."( Pharmacokinetics of quinapril in children: assessment during substitution for chronic angiotensin-converting enzyme inhibitor treatment.
Batisky, D; Blumer, JL; Daniels, SR; Dreyer, WJ; Ouellet, D; Roman, D; Walson, PD, 2003
)
0.92
" Patients who received a full dosage of ACEI did not have to posses an increasing risk of C-ACEI."( Angiotensin converting enzyme inhibitor induced cough: experience in Siriraj Hospital.
Buranakitjaroen, P; Phoojaroenchanachai, M; Sangprasert, P; Saravich, S; Sriussadaporn, S, 2003
)
0.32
" The designed system offers a resource sparing primary screen for drug-excipient chemical compatibility for solid dosage form development."( Design and utilization of the drug-excipient chemical compatibility automated system.
Naath, M; Thomas, VH, 2008
)
0.35
" The developed method was applied successfully for the determination of quinapril in its tablet dosage forms."( Electrochemical behavior of quinapril and its determination in pharmaceutical formulations by square-wave voltammetry at a mercury electrode.
Altinöz, S; Süslü, I, 2008
)
0.87
" Serial plasma concentrations of quinapril and its active metabolite quinaprilat up to 24 h after dosing were determined by HPLC with UV detection."( Pharmacokinetics and bioequivalence study of the two 20-mg quinapril hydrochloride tablet formulations in healthy Thai male volunteers.
Jengjareon, A; Kumsorn, B; Nasangiam, N; Rojanasthien, N; Roongapinun, S, 2008
)
0.87
" High plasma concentrations of gemcabene (>100 microM) achieved in humans and rats upon oral dosing corroborate with gemcabene inhibition of renal OAT3-mediated secretion of quinaprilat in vitro."( Renal organic anion transporter-mediated drug-drug interaction between gemcabene and quinapril.
Bond, BR; Chupka, J; Feng, B; Heath, TG; Yu, Y; Yuan, H; Zheng, JY, 2009
)
0.77
"5 ng/ml) for most horses in the 120 mg dosing group."( Effects of quinapril on angiotensin converting enzyme and plasma renin activity as well as pharmacokinetic parameters of quinapril and its active metabolite, quinaprilat, after intravenous and oral administration to mature horses.
Barlow, BM; Breuhaus, BA; Davis, JL; Kruger, K; LaFevers, DH; Schirmer, JM, 2014
)
0.79
"With a great quantity of solid dosage tested by dissolution technology, developing a rapid and sensitive method to access the content of drug within dissolution media is highly desired by analysts and scientists."( Rapid analysis of drug dissolution by paper spray ionization mass spectrometry.
He, L; Lin, L; Liu, N; Liu, Y; Zhou, YN, 2017
)
0.46
" It is, however, challenging to propose a flexible and robust formulation platform which can be used for fabrication of tailored solid dosage forms composed of APIs with different properties (e."( Binder jetting 3D printing of challenging medicines: From low dose tablets to hydrophobic molecules.
Dominik, A; Górniak, A; Gołkowska, AM; Karolewicz, B; Kozakiewicz-Latała, M; Malec, K; Nartowski, KP; Rusińska, M; Szymczyk-Ziółkowska, P; Ziółkowski, G; Złocińska, A, 2022
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitorAn EC 3.4.15.* (peptidyl-dipeptidase) inhibitor that interferes with the action of peptidyl-dipeptidase A (EC 3.4.15.1).
prodrugA compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.
antihypertensive agentAny drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
isoquinolinesA class of organic heteropolycyclic compound consisting of isoquinoline and its substitution derivatives.
dicarboxylic acid monoesterA monoester of a dicarboxylic acid.
ethyl esterAny carboxylic ester resulting from the formal condensation of the carboxy group of a carboxylic acid with ethanol.
tertiary carboxamideA carboxamide resulting from the formal condensation of a carboxylic acid with a secondary amine; formula RC(=O)NHR(1)R(2).
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency37.90830.01237.983543.2770AID1645841
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)54.75000.11007.190310.0000AID1449628; AID1473738
Angiotensin-converting enzyme Homo sapiens (human)IC50 (µMol)0.00830.00010.533610.0000AID38859; AID39750; AID39758; AID39767
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC50 (µMol)0.11000.00001.612910.0000AID1231572
Angiotensin-converting enzyme 2 Homo sapiens (human)IC50 (µMol)0.00830.00042.207910.0000AID39758
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (129)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
response to hypoxiaAngiotensin-converting enzyme Homo sapiens (human)
kidney developmentAngiotensin-converting enzyme Homo sapiens (human)
blood vessel remodelingAngiotensin-converting enzyme Homo sapiens (human)
angiotensin maturationAngiotensin-converting enzyme Homo sapiens (human)
regulation of renal output by angiotensinAngiotensin-converting enzyme Homo sapiens (human)
neutrophil mediated immunityAngiotensin-converting enzyme Homo sapiens (human)
antigen processing and presentation of peptide antigen via MHC class IAngiotensin-converting enzyme Homo sapiens (human)
regulation of systemic arterial blood pressure by renin-angiotensinAngiotensin-converting enzyme Homo sapiens (human)
proteolysisAngiotensin-converting enzyme Homo sapiens (human)
spermatogenesisAngiotensin-converting enzyme Homo sapiens (human)
female pregnancyAngiotensin-converting enzyme Homo sapiens (human)
regulation of blood pressureAngiotensin-converting enzyme Homo sapiens (human)
male gonad developmentAngiotensin-converting enzyme Homo sapiens (human)
response to xenobiotic stimulusAngiotensin-converting enzyme Homo sapiens (human)
embryo development ending in birth or egg hatchingAngiotensin-converting enzyme Homo sapiens (human)
post-transcriptional regulation of gene expressionAngiotensin-converting enzyme Homo sapiens (human)
negative regulation of gene expressionAngiotensin-converting enzyme Homo sapiens (human)
substance P catabolic processAngiotensin-converting enzyme Homo sapiens (human)
bradykinin catabolic processAngiotensin-converting enzyme Homo sapiens (human)
regulation of smooth muscle cell migrationAngiotensin-converting enzyme Homo sapiens (human)
regulation of vasoconstrictionAngiotensin-converting enzyme Homo sapiens (human)
animal organ regenerationAngiotensin-converting enzyme Homo sapiens (human)
response to nutrient levelsAngiotensin-converting enzyme Homo sapiens (human)
response to lipopolysaccharideAngiotensin-converting enzyme Homo sapiens (human)
mononuclear cell proliferationAngiotensin-converting enzyme Homo sapiens (human)
response to laminar fluid shear stressAngiotensin-converting enzyme Homo sapiens (human)
angiotensin-activated signaling pathwayAngiotensin-converting enzyme Homo sapiens (human)
vasoconstrictionAngiotensin-converting enzyme Homo sapiens (human)
hormone metabolic processAngiotensin-converting enzyme Homo sapiens (human)
hormone catabolic processAngiotensin-converting enzyme Homo sapiens (human)
eating behaviorAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of apoptotic processAngiotensin-converting enzyme Homo sapiens (human)
peptide catabolic processAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of vasoconstrictionAngiotensin-converting enzyme Homo sapiens (human)
negative regulation of glucose importAngiotensin-converting enzyme Homo sapiens (human)
regulation of synaptic plasticityAngiotensin-converting enzyme Homo sapiens (human)
lung alveolus developmentAngiotensin-converting enzyme Homo sapiens (human)
amyloid-beta metabolic processAngiotensin-converting enzyme Homo sapiens (human)
arachidonic acid secretionAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of neurogenesisAngiotensin-converting enzyme Homo sapiens (human)
heart contractionAngiotensin-converting enzyme Homo sapiens (human)
regulation of angiotensin metabolic processAngiotensin-converting enzyme Homo sapiens (human)
hematopoietic stem cell differentiationAngiotensin-converting enzyme Homo sapiens (human)
angiogenesis involved in coronary vascular morphogenesisAngiotensin-converting enzyme Homo sapiens (human)
cellular response to glucose stimulusAngiotensin-converting enzyme Homo sapiens (human)
response to dexamethasoneAngiotensin-converting enzyme Homo sapiens (human)
cell proliferation in bone marrowAngiotensin-converting enzyme Homo sapiens (human)
regulation of heart rate by cardiac conductionAngiotensin-converting enzyme Homo sapiens (human)
negative regulation of calcium ion importAngiotensin-converting enzyme Homo sapiens (human)
response to thyroid hormoneAngiotensin-converting enzyme Homo sapiens (human)
blood vessel diameter maintenanceAngiotensin-converting enzyme Homo sapiens (human)
regulation of hematopoietic stem cell proliferationAngiotensin-converting enzyme Homo sapiens (human)
negative regulation of gap junction assemblyAngiotensin-converting enzyme Homo sapiens (human)
cellular response to aldosteroneAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of peptidyl-cysteine S-nitrosylationAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of systemic arterial blood pressureAngiotensin-converting enzyme Homo sapiens (human)
cholesterol biosynthetic processLiver carboxylesterase 1Homo sapiens (human)
cholesterol metabolic processLiver carboxylesterase 1Homo sapiens (human)
response to toxic substanceLiver carboxylesterase 1Homo sapiens (human)
positive regulation of cholesterol effluxLiver carboxylesterase 1Homo sapiens (human)
negative regulation of cholesterol storageLiver carboxylesterase 1Homo sapiens (human)
epithelial cell differentiationLiver carboxylesterase 1Homo sapiens (human)
cholesterol homeostasisLiver carboxylesterase 1Homo sapiens (human)
reverse cholesterol transportLiver carboxylesterase 1Homo sapiens (human)
medium-chain fatty acid metabolic processLiver carboxylesterase 1Homo sapiens (human)
regulation of bile acid biosynthetic processLiver carboxylesterase 1Homo sapiens (human)
cellular response to cholesterolLiver carboxylesterase 1Homo sapiens (human)
cellular response to low-density lipoprotein particle stimulusLiver carboxylesterase 1Homo sapiens (human)
cholesterol ester hydrolysis involved in cholesterol transportLiver carboxylesterase 1Homo sapiens (human)
positive regulation of cholesterol metabolic processLiver carboxylesterase 1Homo sapiens (human)
regulation of bile acid secretionLiver carboxylesterase 1Homo sapiens (human)
lipid catabolic processLiver carboxylesterase 1Homo sapiens (human)
negative regulation of signaling receptor activityAngiotensin-converting enzyme 2 Homo sapiens (human)
symbiont entry into host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of cytokine productionAngiotensin-converting enzyme 2 Homo sapiens (human)
angiotensin maturationAngiotensin-converting enzyme 2 Homo sapiens (human)
angiotensin-mediated drinking behaviorAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of systemic arterial blood pressure by renin-angiotensinAngiotensin-converting enzyme 2 Homo sapiens (human)
tryptophan transportAngiotensin-converting enzyme 2 Homo sapiens (human)
viral life cycleAngiotensin-converting enzyme 2 Homo sapiens (human)
receptor-mediated endocytosis of virus by host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of vasoconstrictionAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of transmembrane transporter activityAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of cell population proliferationAngiotensin-converting enzyme 2 Homo sapiens (human)
symbiont entry into host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
receptor-mediated virion attachment to host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
negative regulation of smooth muscle cell proliferationAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of inflammatory responseAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of amino acid transportAngiotensin-converting enzyme 2 Homo sapiens (human)
maternal process involved in female pregnancyAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of cardiac muscle contractionAngiotensin-converting enzyme 2 Homo sapiens (human)
membrane fusionAngiotensin-converting enzyme 2 Homo sapiens (human)
negative regulation of ERK1 and ERK2 cascadeAngiotensin-converting enzyme 2 Homo sapiens (human)
blood vessel diameter maintenanceAngiotensin-converting enzyme 2 Homo sapiens (human)
entry receptor-mediated virion attachment to host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of gap junction assemblyAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of cardiac conductionAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of L-proline import across plasma membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processAngiotensin-converting enzyme 2 Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (45)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
endopeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
carboxypeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
metalloendopeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
calmodulin bindingAngiotensin-converting enzyme Homo sapiens (human)
peptidase activityAngiotensin-converting enzyme Homo sapiens (human)
metallopeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
exopeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
tripeptidyl-peptidase activityAngiotensin-converting enzyme Homo sapiens (human)
peptidyl-dipeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
zinc ion bindingAngiotensin-converting enzyme Homo sapiens (human)
chloride ion bindingAngiotensin-converting enzyme Homo sapiens (human)
mitogen-activated protein kinase kinase bindingAngiotensin-converting enzyme Homo sapiens (human)
bradykinin receptor bindingAngiotensin-converting enzyme Homo sapiens (human)
mitogen-activated protein kinase bindingAngiotensin-converting enzyme Homo sapiens (human)
metallodipeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
heterocyclic compound bindingAngiotensin-converting enzyme Homo sapiens (human)
sterol esterase activityLiver carboxylesterase 1Homo sapiens (human)
methylumbelliferyl-acetate deacetylase activityLiver carboxylesterase 1Homo sapiens (human)
carboxylesterase activityLiver carboxylesterase 1Homo sapiens (human)
carboxylic ester hydrolase activityLiver carboxylesterase 1Homo sapiens (human)
virus receptor activityAngiotensin-converting enzyme 2 Homo sapiens (human)
endopeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
carboxypeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
metallocarboxypeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
protein bindingAngiotensin-converting enzyme 2 Homo sapiens (human)
metallopeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
peptidyl-dipeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
zinc ion bindingAngiotensin-converting enzyme 2 Homo sapiens (human)
identical protein bindingAngiotensin-converting enzyme 2 Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (31)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceAngiotensin-converting enzyme Homo sapiens (human)
extracellular regionAngiotensin-converting enzyme Homo sapiens (human)
extracellular spaceAngiotensin-converting enzyme Homo sapiens (human)
lysosomeAngiotensin-converting enzyme Homo sapiens (human)
endosomeAngiotensin-converting enzyme Homo sapiens (human)
plasma membraneAngiotensin-converting enzyme Homo sapiens (human)
external side of plasma membraneAngiotensin-converting enzyme Homo sapiens (human)
basal plasma membraneAngiotensin-converting enzyme Homo sapiens (human)
brush border membraneAngiotensin-converting enzyme Homo sapiens (human)
extracellular exosomeAngiotensin-converting enzyme Homo sapiens (human)
sperm midpieceAngiotensin-converting enzyme Homo sapiens (human)
plasma membraneAngiotensin-converting enzyme Homo sapiens (human)
cytoplasmLiver carboxylesterase 1Homo sapiens (human)
endoplasmic reticulumLiver carboxylesterase 1Homo sapiens (human)
endoplasmic reticulum lumenLiver carboxylesterase 1Homo sapiens (human)
lipid dropletLiver carboxylesterase 1Homo sapiens (human)
cytosolLiver carboxylesterase 1Homo sapiens (human)
lipid dropletLiver carboxylesterase 1Homo sapiens (human)
endoplasmic reticulumLiver carboxylesterase 1Homo sapiens (human)
plasma membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
extracellular regionAngiotensin-converting enzyme 2 Homo sapiens (human)
extracellular spaceAngiotensin-converting enzyme 2 Homo sapiens (human)
endoplasmic reticulum lumenAngiotensin-converting enzyme 2 Homo sapiens (human)
plasma membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
ciliumAngiotensin-converting enzyme 2 Homo sapiens (human)
cell surfaceAngiotensin-converting enzyme 2 Homo sapiens (human)
membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
apical plasma membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
endocytic vesicle membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
brush border membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
membrane raftAngiotensin-converting enzyme 2 Homo sapiens (human)
extracellular exosomeAngiotensin-converting enzyme 2 Homo sapiens (human)
extracellular spaceAngiotensin-converting enzyme 2 Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (73)

Assay IDTitleYearJournalArticle
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID39758Inhibition of guinea pig angiotensin I converting enzyme1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID409953Inhibition of mouse liver MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID186359Baseline mean aortic blood pressure in conscious renal (1clip/2kidney) hypertensive rats at dose 0.3 mg/kg administered orally.1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID186686Maximum change aortic blood pressure in conscious renal (1clip/2kidney) hypertensive rats at dose 3 mg/kg administered orally at 5 hr.1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID186360Baseline mean aortic blood pressure in conscious renal (1clip/2kidney) hypertensive rats at dose 10 mg/kg administered orally.1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1210013Inhibition of recombinant CYP2J2 (unknown origin)-mediated terfenadine hydroxylation assessed as remaining activity at 30 uM after 5 mins by LC-MS analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1210014Inhibition of recombinant CYP2J2 (unknown origin)-mediated astemizole O-demethylation assessed as remaining activity at 30 uM after 5 mins by LC-MS/MS analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID186362Baseline mean aortic blood pressure in conscious renal (1clip/2kidney) hypertensive rats at dose 1 mg/kg administered orally.1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1473835Stimulation of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID174396% Decrease in mean arterial pressure in conscious renal hypertensive rats at a dose of 3 mg/Kg, administered perorally at MAP 190 mmHg1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Synthesis and biological activity of modified peptide inhibitors of angiotensin-converting enzyme.
AID39767Inhibitory activity against angiotensin I converting enzyme (ACE)2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Protease inhibitors: current status and future prospects.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID186366Baseline mean aortic blood pressure in conscious renal (1clip/2kidney) hypertensive rats at dose 3 mg/kg administered orally.1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID186673Maximum change aortic blood pressure in conscious renal (1clip/2kidney) hypertensive rats at dose 1 mg/kg administered orally at 4 hr.1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types.
AID186542Maximum change aortic blood pressure in conscious renal (1clip/2kidney) hypertensive rats at dose 10 mg/kg administered orally at 5 hr1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types.
AID456232Activity at human recombinant CES1 expressed in baculovirus-infected Spodoptera frugiperda Sf21 cells assessed as substrate hydrolysis by fluorescence assay2010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
In silico prediction of human carboxylesterase-1 (hCES1) metabolism combining docking analyses and MD simulations.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID38859Compound was tested for its inhibitory potency against angiotensin I converting enzyme.1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Molecular and crystal structures of MDL27,467A hydrochloride and quinapril hydrochloride, two ester derivatives of potent angiotensin converting enzyme inhibitors.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID186539Maximum change aortic blood pressure in conscious renal (1clip/2kidney) hypertensive rats at dose 0.3 mg/kg administered orally at 10 hr.1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID39750In vitro inhibitory activity against Angiotensin I converting enzyme from unpurified guinea pig serum1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Synthesis and biological activity of modified peptide inhibitors of angiotensin-converting enzyme.
AID1231572Inhibition of rabbit lung ACE assessed as hippuryl-histidyl-leucine hydrolysis after 30 mins by colorimetric method2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Design, synthesis and evaluation of novel 2-butyl-4-chloroimidazole derived peptidomimetics as Angiotensin Converting Enzyme (ACE) inhibitors.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID640615Clearance in human liver microsomes at 1 uM measured after 60 mins by HPLC analysis2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Capture hydrolysis signals in the microsomal stability assay: molecular mechanisms of the alkyl ester drug and prodrug metabolism.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (603)

TimeframeStudies, This Drug (%)All Drugs %
pre-199029 (4.81)18.7374
1990's283 (46.93)18.2507
2000's233 (38.64)29.6817
2010's53 (8.79)24.3611
2020's5 (0.83)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 67.60

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index67.60 (24.57)
Research Supply Index6.77 (2.92)
Research Growth Index5.39 (4.65)
Search Engine Demand Index116.43 (26.88)
Search Engine Supply Index1.99 (0.95)

This Compound (67.60)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials220 (33.74%)5.53%
Reviews42 (6.44%)6.00%
Case Studies25 (3.83%)4.05%
Observational1 (0.15%)0.25%
Other364 (55.83%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (23)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Single-Dose Fasting In Vivo Bioequivalence Study of Quinapril HCl and Hydrochlorothiazide Tablets (20 mg/25 mg; Mylan) to Accuretic™ Tablets (20 mg/25 mg; Parke-Davis) in Healthy Volunteers [NCT00649441]Phase 160 participants (Actual)Interventional2003-08-31Completed
Long - Term Effect of Quinapril or Losartan or Their Combination on Diabetic Autonomic Neuropathy and Left Ventricular Function Over a Period of 4 Years. A Radionuclide Ventriculography Study. [NCT05713396]Phase 459 participants (Actual)Interventional2017-01-01Completed
ASSET (Acupil® Non Interventional Study For Evaluation Of Safety Effectiveness And Tolerability) [NCT00930722]329 participants (Actual)Observational2009-06-30Completed
Association Between Angiotensin Converting Enzyme Inhibitor or Angiotensin Receptor Blocker Use and COVID-19 Severity and Mortality Among US Veterans [NCT04467931]22,213 participants (Actual)Observational2020-01-19Completed
Single-Dose Food In Vivo Bioequivalence Study of Quinapril HCl and Hydrochlorothiazide Tablets (20 mg/25 mg; Mylan) to Accuretic™ Tablets (20 mg/25 mg; Parke-Davis) in Healthy Volunteers [NCT00648011]Phase 144 participants (Actual)Interventional2003-08-31Completed
Single-Dose Food In Vivo Bioequivalence Study of Quinapril Hydrochloride Tablets (40 mg; Mylan) and Accupril® Tablets (40 mg; Parke-Davis) in Healthy Volunteers [NCT00649649]Phase 124 participants (Actual)Interventional2002-12-31Completed
Single-Dose Fasting In Vivo Bioequivalence Study of Quinapril Hydrochloride Tablets (40 mg; Mylan) and Accupril® Tablets (40 mg; Parke-Davis) in Healthy Volunteers [NCT00649103]Phase 160 participants (Actual)Interventional2002-12-31Completed
A 12-Week Open-Label, Uncontrolled Multicenter Study to Assess the Efficacy and Safety of Quinapril or Quinapril Plus Hydrochlorothiazide in Subjects With Mild to Moderate Hypertension [NCT00651287]Phase 4200 participants (Actual)Interventional2002-12-31Completed
A 22-week Randomized, Cross-over Study Comparing the Effects of Quinapril and Quinapril Plus Alpha-lipoic Acid (ALA) on Patients With Diabetes Mellitus and Hypertension [NCT00795262]23 participants (Actual)Interventional2008-07-31Completed
Prognostic Value of the Circadian Pattern of Ambulatory Blood Pressure for Multiple Risk Assessment [NCT00741585]Phase 421,983 participants (Actual)Interventional2008-09-01Completed
NT-proBNP Selected PreventiOn of Cardiac eveNts in a populaTion of dIabetic Patients Without A History of Cardiac Disease: a Prospective Randomized Trial [NCT02817360]Phase 42,400 participants (Anticipated)Interventional2016-02-29Recruiting
An Open Label, Balanced, Randomised, Two-Treatment, Four-Period, Two-Sequence, Single-Dose, Crossover, Fully Replicated Bioavailability Study on Fixed-Dose Combination of Quinapril 20 mg and Hydrochlorothiazide 25 mg Tablets of OHM Laboratories Inc.(Divis [NCT00872235]40 participants (Actual)Interventional2005-06-30Completed
An Open Label, Balanced, Randomized, Two-Treatment, Two-Period, Two-Sequence, Single-Dose, Crossover Bioavailability Study Comparing Fixed Dose Combination of Quinapril HCl 20 mg and Hydrochlorothiazide 25 mg Tablets of OHM Laboratories Inc (a Subsidiary [NCT00872781]64 participants (Actual)Interventional2007-10-31Completed
Multicenter, Open-Label (Non-Comparative) Study To Evaluate Changes In Flow Mediated Dilatation During And After A 6 Months Treatment Period With Step By Step Increased Doses With Quinapril Therapy In Post-Menopausal Women With Mild Or Moderate Hypertensi [NCT00147524]Phase 470 participants Interventional2003-10-31Completed
The CORONAvirus Disease 2019 Angiotensin Converting Enzyme Inhibitor/Angiotensin Receptor Blocker InvestigatiON (CORONACION) Randomized Clinical Trial [NCT04330300]Phase 42,414 participants (Anticipated)Interventional2020-04-30Suspended(stopped due to Challenges with funding and very low incidence of COVID-19 at Irish study site)
[NCT00154050]22 participants Interventional2004-05-31Completed
A Double-Blind, Multicenter, Placebo Controlled Study of Quinapril in Women With Chest Pain, Coronary Flow Reserve Limitations and Evidence of Myocardial Ischemia in the Absence of Significant Epicardial Coronary Artery Disease. [NCT00150826]Phase 478 participants (Actual)Interventional2000-05-31Completed
Chronic Angiotensin Converting Enzyme Inhibitors in Intermediate Risk Surgery: A Randomized, Single-Blinded Study [NCT01669434]Phase 4291 participants (Actual)Interventional2015-06-01Completed
Prognostic Value of Ambulatory Blood Pressure Monitoring in the Prediction of Cardiovascular Events and Effects of Chronotherapy in Relation to Risk (the MAPEC Study). [NCT00295542]Phase 43,344 participants (Actual)Interventional2000-03-31Completed
The Ischemia Management With Accupril Post Bypass Graft Via Inhibition of the coNverting Enzyme (IMAGINE) Trial [NCT00269243]Phase 40 participants Interventional1999-11-30Completed
Impact of High-Dose Quinapril Versus Low-Dose Quinapril Plus Amlodipine on Autonomic Regulation and on Sympathetic Activation in Response to Cold Exposure in Hypertensive Patients With Impaired Glucose Tolerance, Diabetes or Coronary Artery Disease [NCT00313547]Phase 440 participants (Anticipated)Interventional2006-04-30Terminated(stopped due to Very difficult to recruit patients/slow recruitment(2 patients in nearly 2 years).)
Randomised, Double Blind, Placebo Controlled Trial of Angiotensin Converting Enzyme Inhibitors and Statins in the Prevention of Long Term Complications in Young People With Type 1 Diabetes [NCT01581476]Phase 3443 participants (Actual)Interventional2009-01-31Completed
Efficacy of Administration of Angiotensin Converting Enzyme Inhibition on Autonomic and Peripheral Neuropathy in Patients With Diabetes Mellitus [NCT03031834]Phase 40 participants Interventional1999-01-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00930722 (8) [back to overview]Mean Daily Dose of Study Medication
NCT00930722 (8) [back to overview]Number of Participants Achieving BP Goal at Week 12
NCT00930722 (8) [back to overview]Change From Baseline in Diastolic Blood Pressure (DBP) at Week 12
NCT00930722 (8) [back to overview]Change From Baseline in Systolic Blood Pressure (SBP) at Week 12
NCT00930722 (8) [back to overview]Change From Pre-treatment in DBP at Week 0
NCT00930722 (8) [back to overview]Change From Pre-treatment in SBP at Week 0
NCT00930722 (8) [back to overview]Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT00930722 (8) [back to overview]Number of Participants With Preference for add-on Anti-hypertensive Therapy
NCT01669434 (6) [back to overview]Acute Renal Failure
NCT01669434 (6) [back to overview]Low Blood Pressure Subgroup
NCT01669434 (6) [back to overview]Number of Participants With Interoperative Hypotension
NCT01669434 (6) [back to overview]Older Age Subgroup
NCT01669434 (6) [back to overview]Postoperative Hypertension
NCT01669434 (6) [back to overview]Postoperative Hypotension

Mean Daily Dose of Study Medication

The mean daily dose of the study medication was calculated by dividing the total dose (sum of the daily doses) in the study by the treatment duration. (NCT00930722)
Timeframe: Baseline up to week 52 or early termination

Interventionmg (Mean)
Quinapril11.28

[back to top]

Number of Participants Achieving BP Goal at Week 12

"The status of achieving a participant's goal BP at Week 12 was yes (at goal) or no (not at goal). The BP goal also depended on the participant's status of Diabetes Mellitus (DM) or renal disease. To be considered at goal, SBP/DBP must be less than 140/90 mmHg for participants without DM or renal disease and SBP/DBP must be less than 130/80 mmHg for participants with DM or renal disease." (NCT00930722)
Timeframe: Week 12

InterventionParticipants (Number)
Quinapril78

[back to top]

Change From Baseline in Diastolic Blood Pressure (DBP) at Week 12

Value at week 12 minus value at baseline. (NCT00930722)
Timeframe: Baseline and Week 12

InterventionmmHg (Mean)
BaselineChange at Week 12
Quinapril86.31-3.93

[back to top]

Change From Baseline in Systolic Blood Pressure (SBP) at Week 12

Value at week 12 minus value at baseline. (NCT00930722)
Timeframe: Baseline and Week 12

InterventionMillimeters of mercury (mmHg) (Mean)
BaselineChange at Week 12
Quinapril142.16-9.40

[back to top]

Change From Pre-treatment in DBP at Week 0

Value at Week 0 minus value at pre-treatment. Pre-treatment BP was the last BP recorded before taking study medication from retrospective data. If no such value was available, the earliest retrospective BP value from medical records was considered. (NCT00930722)
Timeframe: Pre-treatment and Week 0

InterventionmmHg (Mean)
Pre-treatmentChange at Week 0
Quinapril92.82-6.74

[back to top]

Change From Pre-treatment in SBP at Week 0

Value at Week 0 minus value at pre-treatment. Pre-treatment BP was the last BP recorded before taking study medication from retrospective data. If no such value was available, the earliest retrospective BP value from medical records was considered. (NCT00930722)
Timeframe: Pre-treatment and Week 0

InterventionmmHg (Mean)
Pre-treatmentChange at Week 0
Quinapril154.06-12.49

[back to top]

Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)

Any untoward medical occurrence in a participant who received study drug was considered an AE, without regard to possibility of causal relationship. Treatment-emergent adverse events (TEAE): those which occurred or worsened after baseline. An AE resulting in any of the following outcomes, or deemed to be significant for any other reason, was considered to be a SAE: death; initial or prolonged inpatient hospitalization; a life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. (NCT00930722)
Timeframe: Baseline to Week 52

InterventionParticipants (Number)
Adverse eventsSerious adverse events
Quinapril10

[back to top]

Number of Participants With Preference for add-on Anti-hypertensive Therapy

"The first add-on antihypertensive therapy for each participant was the first additional antihypertensive medication since initiation of Quinapril. If the participant did not require any such add-on medication, the first add-on antihypertensive therapy was None." (NCT00930722)
Timeframe: Baseline up to week 52 or early termination

InterventionParticipants (Number)
NoneMetoprololMetoprolol Succinate
Quinapril32111

[back to top]

Acute Renal Failure

Creatinine increase of more than 0.3 mg/dl or more than 50% from preoperative level (NCT01669434)
Timeframe: Arrival in post-anesthesia care unit (PACU) to hospital discharge, an expected average of 4 days.

InterventionParticipants (Count of Participants)
ACEI Omission6
ACEI Continuation10

[back to top]

Low Blood Pressure Subgroup

Only patients with systolic blood pressure less than 110 at preoperative evaluation will be included in this analysis. The outcome is the same as the primary outcome: Intraoperative Systolic Blood Pressure under 80 mmHg. (NCT01669434)
Timeframe: During anesthesia, an expected average of 3 hours.

InterventionParticipants (Count of Participants)
ACEI Omission4
ACEI Continuation2

[back to top]

Number of Participants With Interoperative Hypotension

Number of Participants with Interoperative Hypotension (systolic blood pressure under 80 mmHg) (NCT01669434)
Timeframe: During anesthesia, an expected average of 3 hours.

InterventionParticipants (Count of Participants)
ACEI Omission76
ACEI Continuation95

[back to top]

Older Age Subgroup

Only patients above the age of 64 will be included in this analysis. The outcome is the same as the primary outcome: Intraoperative Systolic Blood Pressure under 80 mmHg (NCT01669434)
Timeframe: During anesthesia, an expected average of 3 hours.

InterventionParticipants (Count of Participants)
ACEI Omission48
ACEI Continuation49

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Postoperative Hypertension

Any systolic blood pressure greater than 180 mmHg. (NCT01669434)
Timeframe: Arrival in PACU to hospital discharge, an expected average of 4 days.

InterventionParticipants (Count of Participants)
ACEI Omission33
ACEI Continuation17

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Postoperative Hypotension

Any systolic blood pressure less than 90 mmHg (NCT01669434)
Timeframe: Arrival in PACU to hospital discharge, an expected average of 4 days.

InterventionParticipants (Count of Participants)
ACEI Omission15
ACEI Continuation31

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