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[PMID]:27670279
[Au] Autor:Okawada M; Wilson MW; Larsen SD; Lipka E; Hillfinger J; Teitelbaum DH
[Ad] Endereço:Section of Pediatric Surgery, Department of Surgery, The University of Michigan Medical School, Mott Children's Hospital, F3970, Ann Arbor, MI, 48109-0245, USA. manabu-o@juntendo.ac.jp.
[Ti] Título:Blockade of the renin-angiotensin system prevents acute and immunologically relevant colitis in murine models.
[So] Source:Pediatr Surg Int;32(12):1103-1114, 2016 Dec.
[Is] ISSN:1437-9813
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Blockade of the renin-angiotensin system (RAS) has been shown to alleviate inflammatory processes in the gastrointestinal tract. The aim of this study was to determine if blockade of the RAS would be effective in an immunologically relevant colitis model, and to compare outcome with an acute colitis model. METHODS: A losartan analog, CCG-203025 (C H ClN O S) containing a highly polar sulfonic acid moiety that we expected would allow localized mucosal antagonism with minimal systemic absorption was selected as an angiotensin II type 1a receptor antagonist (AT1aR-A). Two colitis models were studied: (1) Acute colitis was induced in 8- to 10-week-old C57BL/6J mice by 2.5 % dextran sodium sulfate (DSS, in drinking water) for 7 days. (2) IL10-/-colitis Piroxicam (200 ppm) was administered orally in feed to 5-week-old IL-10-/-mice (C57BL/6J background) for 14 days followed by enalaprilat (ACE-I), CCG-203025 or PBS administered transanally for 14 days. RESULTS: In the DSS model, weight loss and histologic score for CCG-203025 were better than with placebo. In the IL10-/-model, ACE-I suppressed histologic damage better than CCG-203025. Both ACE-I and CCG-203025 reduced pro-inflammatory cytokines and chemokines. CONCLUSIONS: This study demonstrated the therapeutic efficacy of both ACE-I and AT1aR-A for preventing the development of both acute and immunologically relevant colitis.
[Mh] Termos MeSH primário: Colite/imunologia
Colite/prevenção & controle
Losartan/análogos & derivados
Losartan/farmacologia
Sistema Renina-Angiotensina/efeitos dos fármacos
[Mh] Termos MeSH secundário: Doença Aguda
Bloqueadores do Receptor Tipo 1 de Angiotensina II/imunologia
Bloqueadores do Receptor Tipo 1 de Angiotensina II/farmacologia
Inibidores da Enzima Conversora de Angiotensina/imunologia
Inibidores da Enzima Conversora de Angiotensina/farmacologia
Animais
Colite/patologia
Inibidores de Ciclo-Oxigenase/imunologia
Inibidores de Ciclo-Oxigenase/farmacologia
Modelos Animais de Doenças
Enalaprilate/imunologia
Enalaprilate/farmacologia
Losartan/imunologia
Camundongos
Camundongos Endogâmicos C57BL
Piroxicam/imunologia
Piroxicam/farmacologia
Sistema Renina-Angiotensina/imunologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Angiotensin II Type 1 Receptor Blockers); 0 (Angiotensin-Converting Enzyme Inhibitors); 0 (Cyclooxygenase Inhibitors); 13T4O6VMAM (Piroxicam); GV0O7ES0R3 (Enalaprilat); JMS50MPO89 (Losartan)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170926
[Lr] Data última revisão:
170926
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160928
[St] Status:MEDLINE


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[PMID]:27500599
[Au] Autor:Dahlgren D; Roos C; Johansson P; Lundqvist A; Tannergren C; Abrahamsson B; Sjögren E; Lennernäs H
[Ad] Endereço:Department of Pharmacy, Uppsala University , Uppsala SE-751 23, Sweden.
[Ti] Título:Regional Intestinal Permeability in Dogs: Biopharmaceutical Aspects for Development of Oral Modified-Release Dosage Forms.
[So] Source:Mol Pharm;13(9):3022-33, 2016 Sep 06.
[Is] ISSN:1543-8392
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The development of oral modified-release (MR) dosage forms requires an active pharmaceutical ingredient (API) with a sufficiently high absorption rate in both the small and large intestine. Dogs are commonly used in preclinical evaluation of regional intestinal absorption and in the development of novel MR dosage forms. This study determined regional intestinal effective permeability (Peff) in dogs with the aim to improve regional Peff prediction in humans. Four model drugs, atenolol, enalaprilat, metoprolol, and ketoprofen, were intravenously and regionally dosed twice as a solution into the proximal small intestine (P-SI) and large intestine (LI) of three dogs with intestinal stomas. Based on plasma data from two separate study occasions for each dog, regional Peff values were calculated using a validated intestinal deconvolution method. The determined mean Peff values were 0.62, 0.14, 1.06, and 3.66 × 10(-4) cm/s in the P-SI, and 0.13, 0.02, 1.03, and 2.20 × 10(-4) cm/s in the LI, for atenolol, enalaprilat, metoprolol, and ketoprofen, respectively. The determined P-SI Peff values in dog were highly correlated (R(2) = 0.98) to the historically directly determined human jejunal Peff after a single-pass perfusion. The determined dog P-SI Peff values were also successfully implemented in GI-Sim to predict the risk for overestimation of LI absorption of low permeability drugs. We conclude that the dog intestinal stoma model is a useful preclinical tool for determination of regional intestinal permeability. Still, further studies are recommended to evaluate additional APIs, sources of variability, and formulation types, for more accurate determination of the dog model in the drug development process.
[Mh] Termos MeSH primário: Intestino Grosso/metabolismo
Intestino Delgado/metabolismo
[Mh] Termos MeSH secundário: Animais
Atenolol/farmacocinética
Cães
Enalaprilate/farmacocinética
Seres Humanos
Absorção Intestinal
Jejuno/metabolismo
Cetoprofeno/farmacocinética
Masculino
Metoprolol/farmacocinética
Permeabilidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
50VV3VW0TI (Atenolol); 90Y4QC304K (Ketoprofen); GEB06NHM23 (Metoprolol); GV0O7ES0R3 (Enalaprilat)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171020
[Lr] Data última revisão:
171020
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160809
[St] Status:MEDLINE
[do] DOI:10.1021/acs.molpharmaceut.6b00515


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[PMID]:27344631
[Au] Autor:Bouabdallah S; Ben Dhia MT; Driss MR; Touil S
[Ad] Endereço:Laboratory of Heteroatom Organic Chemistry, Department of Chemistry, Faculty of Sciences of Bizerte, University of Carthage, 7021 Jarzouna, Tunisia. Electronic address: sondes.bouabdallah@laposte.net.
[Ti] Título:Investigation of the energy barrier to the rotation of amide CN bonds in ACE inhibitors by NMR, dynamic HPLC and DFT.
[So] Source:J Pharm Biomed Anal;128:416-425, 2016 Sep 05.
[Is] ISSN:1873-264X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The isomerizations of Enalapril, Perindopril, Enalaprilat and Lisinopril have been investigated using NMR spectroscopic, dynamic chromatographic, unified equation and DFT theoretical calculations. The thermodynamic parameters (ΔH, ΔS and ΔG) were determined by varying the temperature in the NMR experiments. At the coalescence temperature, we can evaluate the isomerization barrier to the rotation (ΔG(≠)) around the amide bond. Using dynamics chromatography and an unified equation introduced by Trap, we can determine isomerization rate constants and Gibbs activation energies. Molecular mechanics calculations also provided evidence for the presence of low energy conformers for the ACE due to restricted amide rotation. With the value of barriers (ΔE) between them of the order of (20kJmol(-1)), which is in agreement with the dynamic NMR results and DFT calculations.
[Mh] Termos MeSH primário: Inibidores da Enzima Conversora de Angiotensina/química
Cromatografia Líquida de Alta Pressão
Espectroscopia de Ressonância Magnética
[Mh] Termos MeSH secundário: Amidas/química
Enalapril/química
Enalaprilate/química
Isomerismo
Lisinopril/química
Modelos Estatísticos
Perindopril/química
Termodinâmica
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amides); 0 (Angiotensin-Converting Enzyme Inhibitors); 69PN84IO1A (Enalapril); E7199S1YWR (Lisinopril); GV0O7ES0R3 (Enalaprilat); Y5GMK36KGY (Perindopril)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170812
[Lr] Data última revisão:
170812
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160627
[St] Status:MEDLINE


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[PMID]:26729306
[Au] Autor:Boustany-Kari CM; Harrison PC; Chen H; Lincoln KA; Qian HS; Clifford H; Wang H; Zhang X; Gueneva-Boucheva K; Bosanac T; Wong D; Fryer RM; Richman JG; Sarko C; Pullen SS
[Ad] Endereço:Departments of Cardiometabolic Diseases Research (C.M.B.-K., P.C.H., H.C., K.A.L., H.S.Q., H.C., H.W., X.Z., R.M.F., J.G.R., S.S.P.) and Small Molecule Discovery Research (K.G.-B., T.B., D.W., C.S.), Boehringer Ingelheim Pharmaceuticals, Ridgefield, Connecticut carine.boustany@boehringer-ingelheim.c
[Ti] Título:A Soluble Guanylate Cyclase Activator Inhibits the Progression of Diabetic Nephropathy in the ZSF1 Rat.
[So] Source:J Pharmacol Exp Ther;356(3):712-9, 2016 Mar.
[Is] ISSN:1521-0103
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Therapies that restore renal cGMP levels are hypothesized to slow the progression of diabetic nephropathy. We investigated the effect of BI 703704, a soluble guanylate cyclase (sGC) activator, on disease progression in obese ZSF1 rats. BI 703704 was administered at doses of 0.3, 1, 3, and 10 mg/kg/d to male ZSF1 rats for 15 weeks, during which mean arterial pressure (MAP), heart rate (HR), and urinary protein excretion (UPE) were determined. Histologic assessment of glomerular and interstitial lesions was also performed. Renal cGMP levels were quantified as an indicator of target modulation. BI 703704 resulted in sGC activation, as evidenced by dose-dependent increases in renal cGMP levels. After 15 weeks of treatment, sGC activation resulted in dose-dependent decreases in UPE (from 463 ± 58 mg/d in vehicle controls to 328 ± 55, 348 ± 23, 283 ± 45, and 108 ± 23 mg/d in BI 703704-treated rats at 0.3, 1, 3, and 10 mg/kg, respectively). These effects were accompanied by a significant reduction in the incidence of glomerulosclerosis and interstitial lesions. Decreases in MAP and increases in HR were only observed at the high dose of BI 703704. These results are the first demonstration of renal protection with sGC activation in a nephropathy model induced by type 2 diabetes. Importantly, beneficial effects were observed at doses that did not significantly alter MAP and HR.
[Mh] Termos MeSH primário: Nefropatias Diabéticas/tratamento farmacológico
Nefropatias Diabéticas/enzimologia
Progressão da Doença
Ativadores de Enzimas/farmacologia
Guanilato Ciclase/metabolismo
Receptores Citoplasmáticos e Nucleares/metabolismo
[Mh] Termos MeSH secundário: Animais
Diabetes Mellitus Tipo 2/tratamento farmacológico
Diabetes Mellitus Tipo 2/enzimologia
Enalaprilate/química
Enalaprilate/farmacologia
Enalaprilate/uso terapêutico
Ativadores de Enzimas/química
Ativadores de Enzimas/uso terapêutico
Masculino
Ratos
Ratos Zucker
Guanilil Ciclase Solúvel
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Enzyme Activators); 0 (Receptors, Cytoplasmic and Nuclear); EC 4.6.1.2 (Guanylate Cyclase); EC 4.6.1.2 (Soluble Guanylyl Cyclase); GV0O7ES0R3 (Enalaprilat)
[Em] Mês de entrada:1606
[Cu] Atualização por classe:161126
[Lr] Data última revisão:
161126
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160106
[St] Status:MEDLINE
[do] DOI:10.1124/jpet.115.230706


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[PMID]:26147389
[Au] Autor:Goupil R; Cowley D; Wolley M; Ahmed AH; Gordon RD; Stowasser M
[Ad] Endereço:aEndocrine Hypertension Research Centre, University of Queensland School of Medicine, Greenslopes and Princess Alexandra Hospitals, Brisbane, Queensland, Australia bHôpital du Sacré-Coeur de Montréal, University of Montreal, Montreal, Quebec, Canada.
[Ti] Título:The utility of renal venous renin studies in selection of patients with renal artery stenosis for angioplasty: a retrospective study.
[So] Source:J Hypertens;33(9):1931-8; discussion 1938, 2015 Sep.
[Is] ISSN:1473-5598
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:OBJECTIVES: Recent studies of renal artery stenosis (RAS) failed to demonstrate greater benefit from angioplasty in terms of blood pressure (BP) lowering than medical treatment. Not all RAS are haemodynamically significant and identification of patients likely to benefit from angioplasty remains essential. METHODS: We examined whether performing renal venous renin studies under stringent conditions might predict BP improvement. Patients with at least 60% RAS who underwent renal venous renin measurements in 2008-2013 were identified. Renal venous renin lateralization ratios (RVRRs) were calculated by dividing venous renin from the stenotic kidney with contralateral levels before and after stimulation with enalaprilat or captopril. Benefit was defined as BP less than 140/90  mmHg without medication, 10% decreased mean BP without increased daily defined doses (DDDs) or decreased DDD without a significant increase of mean BP. RESULTS: Twenty-eight patients were treated medically and 42 with angioplasty (median age 60.1 years, 41% male, 29% chronic kidney disease, 50% resistant hypertension). At 11.4 ±â€Š3.3 months, 69% of patients treated with angioplasty had BP benefit compared with 25% with medical treatment (P < 0.001). Logistic regression identified resistant hypertension [odds ratio (OR) 0.18, 95% confidence interval (95% CI) 0.04-0.82, P = 0.03] and baseline DDD (OR 0.69, 95% CI 0.48-0.98, P = 0.04) as being negatively associated, and positive stimulated RVRR (OR 21.6, 95% CI 3.50-133.3, P = 0.001) positively associated with benefit from angioplasty. On multivariate logistic regression, only stimulated RVRR positivity predicted BP benefit (OR 20.5, 95% CI 2.9-145.0, P = 0.003). CONCLUSION: These findings suggest that a positive stimulated RVRR measured under optimal conditions may help to identify patients with RAS likely to improve from angioplasty.
[Mh] Termos MeSH primário: Angioplastia
Obstrução da Artéria Renal/sangue
Renina/sangue
[Mh] Termos MeSH secundário: Idoso
Inibidores da Enzima Conversora de Angiotensina/uso terapêutico
Captopril/uso terapêutico
Enalaprilate/uso terapêutico
Feminino
Seres Humanos
Rim/fisiopatologia
Masculino
Meia-Idade
Obstrução da Artéria Renal/tratamento farmacológico
Obstrução da Artéria Renal/fisiopatologia
Obstrução da Artéria Renal/cirurgia
Estudos Retrospectivos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Angiotensin-Converting Enzyme Inhibitors); 9G64RSX1XD (Captopril); EC 3.4.23.15 (Renin); GV0O7ES0R3 (Enalaprilat)
[Em] Mês de entrada:1604
[Cu] Atualização por classe:150806
[Lr] Data última revisão:
150806
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150707
[St] Status:MEDLINE
[do] DOI:10.1097/HJH.0000000000000635


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[PMID]:25919042
[Au] Autor:Tarkiainen EK; Tornio A; Holmberg MT; Launiainen T; Neuvonen PJ; Backman JT; Niemi M
[Ad] Endereço:Department of Clinical Pharmacology, University of Helsinki and Helsinki University Hospital, Helsinki, Finland.
[Ti] Título:Effect of carboxylesterase 1 c.428G > A single nucleotide variation on the pharmacokinetics of quinapril and enalapril.
[So] Source:Br J Clin Pharmacol;80(5):1131-8, 2015 Nov.
[Is] ISSN:1365-2125
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:AIM: The aim of the present study was to investigate the effects of the carboxylesterase 1 (CES1) c.428G > A (p.G143E, rs71647871) single nucleotide variation (SNV) on the pharmacokinetics of quinapril and enalapril in a prospective genotype panel study in healthy volunteers. METHODS: In a fixed-order crossover study, 10 healthy volunteers with the CES1 c.428G/A genotype and 12 with the c.428G/G genotype ingested a single 10 mg dose of quinapril and enalapril with a washout period of at least 1 week. Plasma concentrations of quinapril and quinaprilat were measured for up to 24 h and those of enalapril and enalaprilat for up to 48 h. Their excretion into the urine was measured from 0 h to 12 h. RESULTS: The area under the plasma concentration-time curve from 0 h to infinity (AUC0-∞) of active enalaprilat was 20% lower in subjects with the CES1 c.428G/A genotype than in those with the c.428G/G genotype (95% confidence interval of geometric mean ratio 0.64, 1.00; P = 0.049). The amount of enalaprilat excreted into the urine was 35% smaller in subjects with the CES1 c.428G/A genotype than in those with the c.428G/G genotype (P = 0.044). 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. The CES1 genotype had no significant effect on the pharmacokinetic or pharmacodynamic parameters of quinapril. CONCLUSIONS: The CES1 c.428G > A SNV decreased enalaprilat concentrations, probably by reducing the hydrolysis of enalapril, but had no observable effect on the pharmacokinetics of quinapril.
[Mh] Termos MeSH primário: Hidrolases de Éster Carboxílico/genética
Enalapril/farmacocinética
Polimorfismo de Nucleotídeo Único/genética
Tetra-Hidroisoquinolinas/farmacocinética
[Mh] Termos MeSH secundário: Adulto
Inibidores da Enzima Conversora de Angiotensina/sangue
Inibidores da Enzima Conversora de Angiotensina/farmacocinética
Inibidores da Enzima Conversora de Angiotensina/farmacologia
Inibidores da Enzima Conversora de Angiotensina/urina
Pressão Sanguínea/efeitos dos fármacos
Estudos Cross-Over
Enalapril/sangue
Enalapril/farmacologia
Enalapril/urina
Enalaprilate/sangue
Enalaprilate/urina
Feminino
Genótipo
Voluntários Saudáveis
Frequência Cardíaca/efeitos dos fármacos
Seres Humanos
Masculino
Tetra-Hidroisoquinolinas/sangue
Tetra-Hidroisoquinolinas/farmacologia
Tetra-Hidroisoquinolinas/urina
Adulto Jovem
[Pt] Tipo de publicação:CLINICAL TRIAL; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Angiotensin-Converting Enzyme Inhibitors); 0 (Tetrahydroisoquinolines); 34SSX5LDE5 (quinaprilat); 69PN84IO1A (Enalapril); EC 3.1.1.- (Carboxylic Ester Hydrolases); EC 3.1.1.1 (CES1 protein, human); GV0O7ES0R3 (Enalaprilat); RJ84Y44811 (quinapril)
[Em] Mês de entrada:1609
[Cu] Atualização por classe:161101
[Lr] Data última revisão:
161101
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150429
[St] Status:MEDLINE
[do] DOI:10.1111/bcp.12667


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[PMID]:25663023
[Au] Autor:Matus M; Kucerova D; Kruzliak P; Adameova A; Doka G; Turcekova K; Kmecova J; Kyselovic J; Krenek P; Kirchhefer U; Mueller FU; Boknik P; Klimas J
[Ad] Endereço:Department of Pharmacology and Toxicology, Faculty of Pharmacy, Comenius University, Bratislava, Slovak Republic.
[Ti] Título:Upregulation of SERCA2a following short-term ACE inhibition (by enalaprilat) alters contractile performance and arrhythmogenicity of healthy myocardium in rat.
[So] Source:Mol Cell Biochem;403(1-2):199-208, 2015 May.
[Is] ISSN:1573-4919
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Chronic angiotensin-converting enzyme inhibitor (ACEIs) treatment can suppress arrhythmogenesis. To examine whether the effect is more immediate and independent of suppression of pathological remodelling, we tested the antiarrhythmic effect of short-term ACE inhibition in healthy normotensive rats. Wistar rats were administered with enalaprilat (ENA, i.p., 5 mg/kg every 12 h) or vehicle (CON) for 2 weeks. Intraarterial blood pressure in situ was measured in A. carotis. Cellular shortening was measured in isolated, electrically paced cardiomyocytes. Standard 12-lead electrocardiography was performed, and hearts of anaesthetized open-chest rats were subjected to 6-min ischemia followed by 10-min reperfusion to examine susceptibility to ventricular arrhythmias. Expressions of calcium-regulating proteins (SERCA2a, cardiac sarco/endoplasmic reticulum Ca(2+)-ATPase; CSQ, calsequestrin; TRD, triadin; PLB, phospholamban; Thr(17)-PLB-phosphorylated PLB at threonine-17, FKBP12.6, FK506-binding protein, Cav1.2-voltage-dependent L-type calcium channel alpha 1C subunit) were measured by Western blot; mRNA levels of L-type calcium channel (Cacna1c), ryanodine receptor (Ryr2) and potassium channels Kcnh2 and Kcnq1 were measured by qRT-PCR. ENA decreased intraarterial systolic as well as diastolic blood pressure (by 20%, and by 31%, respectively, for both P < 0.05) but enhanced shortening of cardiomyocytes at basal conditions (by 34%, P < 0.05) and under beta-adrenergic stimulation (by 73%, P < 0.05). Enalaprilat shortened QTc interval duration (CON 78 ± 1 ms vs. ENA 72 ± 2 ms; P < 0.05) and significantly decreased the total duration of ventricular fibrillations (VF) and the number of VF episodes (P < 0.05). Reduction in arrhythmogenesis was associated with a pronounced upregulation of SERCA2a (CON 100 ± 20 vs. ENA 304 ± 13; P < 0.05) and complete absence of basal Ca(2+)/calmodulin-dependent phosphorylation of PLB at Thr(17). Short-term ACEI treatment can provide protection against I/R injury-induced ventricular arrhythmias in healthy myocardium, and this effect is associated with increased SERCA2a expression.
[Mh] Termos MeSH primário: Inibidores da Enzima Conversora de Angiotensina/farmacologia
Arritmias Cardíacas/fisiopatologia
Enalaprilate/farmacologia
Contração Miocárdica/efeitos dos fármacos
Miocárdio/enzimologia
ATPases Transportadoras de Cálcio do Retículo Sarcoplasmático/genética
Regulação para Cima/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Arritmias Cardíacas/complicações
Arritmias Cardíacas/diagnóstico por imagem
Western Blotting
Canais de Cálcio Tipo L/genética
Canais de Cálcio Tipo L/metabolismo
Separação Celular
Eletrólitos/sangue
Enalaprilate/administração & dosagem
Ventrículos do Coração/efeitos dos fármacos
Ventrículos do Coração/patologia
Ventrículos do Coração/fisiopatologia
Isoproterenol/farmacologia
Masculino
Miocárdio/patologia
Miócitos Cardíacos/efeitos dos fármacos
Miócitos Cardíacos/metabolismo
Miócitos Cardíacos/patologia
Tamanho do Órgão/efeitos dos fármacos
Canais de Potássio/genética
Canais de Potássio/metabolismo
RNA Mensageiro/genética
RNA Mensageiro/metabolismo
Ratos Wistar
Traumatismo por Reperfusão/complicações
Traumatismo por Reperfusão/patologia
Traumatismo por Reperfusão/fisiopatologia
ATPases Transportadoras de Cálcio do Retículo Sarcoplasmático/metabolismo
Ultrassonografia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Angiotensin-Converting Enzyme Inhibitors); 0 (Cacna1c protein, rat); 0 (Calcium Channels, L-Type); 0 (Electrolytes); 0 (Potassium Channels); 0 (RNA, Messenger); EC 3.6.3.8 (Sarcoplasmic Reticulum Calcium-Transporting ATPases); GV0O7ES0R3 (Enalaprilat); L628TT009W (Isoproterenol)
[Em] Mês de entrada:1512
[Cu] Atualização por classe:171030
[Lr] Data última revisão:
171030
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150210
[St] Status:MEDLINE
[do] DOI:10.1007/s11010-015-2350-1


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[PMID]:25224238
[Au] Autor:Chen Y; Song F; Lu G; Lu Z
[Ad] Endereço:Pediatric Critical Care Center, Children's Hospital of Fudan University, Shanghai 201102, China.
[Ti] Título:[Protective effect of an angiotensin-converting-enzyme inhibitor on neurogenic pulmonary edema in rabbits].
[So] Source:Zhonghua Er Ke Za Zhi;52(8):602-6, 2014 Aug.
[Is] ISSN:0578-1310
[Cp] País de publicação:China
[La] Idioma:chi
[Ab] Resumo:OBJECTIVE: Neurogenic pulmonary edema (NPE ) was indicative of poor prognosis in the epidemic of enterovirus 71 infections. The pathogenesis of NPE remains poorly understood. The objectives of this experimental study were to explore whether RAS is activated during NPE in rabbit models induced by fibrin and the effects of an angiotensin converting enzyme inhibitor (enalaprilat) on NPE. METHOD: NPE models were induced by intracisternal injection of fibrinogen and thrombin. According to random number table method, 18 healthy adult New Zealand rabbits were assigned to three groups (with 6 in each) : normal control group (Con group), NPE group and enalaprilat treated (Ena) group. After establishment of NPE models, rabbits in Ena group were given intravenous enalaprilat 0.5 mg/kg. Expression of ACE,ACE2,AT1R mRNA of the lung tissue were evaluated by real-time polymerise chain reaction; and Ang II of the lung tissue was determined by enzyme linked immunosorbent assay ( ELISA ). Meanwhile, histopathological lung injury scores were evaluated. RESULT: ACE mRNA expression level in NPE group ( 17.2 ± 3.3) appeared an increasing trend in contrast to Con group ( 12.6 ± 5.2 ) and Ena group ( 11.5 ± 2.4, both P > 0.05 ). Compared with Con group (81 ± 22 ), ACE2 mRNA expression levels of NPE group ( 52 ± 6 ) and Ena group ( 45 ± 13 ) both decreased ( both P < 0.05 ) . ACE mRNA/ACE2 mRNA expression levels of NPE group ( 0.33 ± 0.06 ) and Ena group ( 0.26 ± 0.04 ) were higher than those of Con group ( 0.16 ± 0.05, both P < 0.05 ), as well as the ratio of Ena group decreased compared with untreated NPE group ( 0.26 ± 0.04 vs. 0.33 ± 0.06, P < 0.05 ) . There were no statistically significant differences in expression of AT1 mRNA of the lung tissue among three groups, but Ena group ( 4.8 ± 1.1) in contrast to NPE group ( 6.7 ± 1.3) has no significant difference (P > 0.05). Lung AngII level of NPE group [(540 ± 147) pg/ml] was significantly higher than that of Con group [(253 ± 37 ) pg/ml] and Ena group [(309 ± 35 ) pg/ml, both P < 0.05 ]. Gross pathologic examination showed that pink foamy edema fluid appeared in the tracheal tubes in NPE group, but spontaneously appeared in neither Con group nor Ena group; and the level of pulmonary subpleural bleeding in Con group, 12 graded 0; in NPE group, 2 graded II, 10 graded III; in Ena group, 2 graded, 8 grade II, 2 grade III. The histopathologic lung injury scores in Ena group was decreased in contrast to NPE group (1.36 ± 0.26 vs.2.32 ± 0.49, P < 0.05) and mainly for the improvement of alveolar overdistension and interstitial edema. CONCLUSION: The present study showed that when NPE occurs, a high lung AngII concentration was associated with an imbalance between ACE mRNA to ACE2 mRNA expression level. Activated local RAS in lung tissue resulted in lung injury. Enalaprilat treatment may attenuate lung injury by interventing local RAS in lung tissue with decreased ratio of ACE mRNA to ACE2 mRNA and lung AngII concentration. The result will be significant for the angiotensin converting enzyme inhibitor used in the theatment of NPE.
[Mh] Termos MeSH primário: Angiotensina II/metabolismo
Inibidores da Enzima Conversora de Angiotensina/farmacologia
Enalaprilate/farmacologia
Peptidil Dipeptidase A/metabolismo
Edema Pulmonar/metabolismo
[Mh] Termos MeSH secundário: Angiotensina II/genética
Animais
Modelos Animais de Doenças
Feminino
Fibrinogênio/farmacologia
Regulação Enzimológica da Expressão Gênica
Pulmão/metabolismo
Pulmão/patologia
Masculino
Peptidil Dipeptidase A/genética
Edema Pulmonar/induzido quimicamente
Edema Pulmonar/patologia
RNA Mensageiro/metabolismo
Coelhos
Distribuição Aleatória
Reação em Cadeia da Polimerase em Tempo Real
[Pt] Tipo de publicação:ENGLISH ABSTRACT; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Angiotensin-Converting Enzyme Inhibitors); 0 (RNA, Messenger); 11128-99-7 (Angiotensin II); 9001-32-5 (Fibrinogen); EC 3.4.15.1 (Peptidyl-Dipeptidase A); GV0O7ES0R3 (Enalaprilat)
[Em] Mês de entrada:1501
[Cu] Atualização por classe:160607
[Lr] Data última revisão:
160607
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140917
[St] Status:MEDLINE


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[PMID]:24972864
[Au] Autor:Gómez-Díez M; Muñoz A; Caballero JM; Riber C; Castejón F; Serrano-Rodríguez JM
[Ad] Endereço:Equine Sport Medicine Centre, CEMEDE, School of Veterinary Medicine, University of Córdoba, Spain.
[Ti] Título:Pharmacokinetics and pharmacodynamics of enalapril and its active metabolite, enalaprilat, at four different doses in healthy horses.
[So] Source:Res Vet Sci;97(1):105-10, 2014 Aug.
[Is] ISSN:1532-2661
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Pharmacokinetic and pharmacodynamic of IV enalapril at 0.50 mg/kg, PO placebo and PO enalapril at three different doses (0.50, 1.00 and 2.00 mg/kg) were analyzed in 7 healthy horses. Serum concentrations of enalapril and enalaprilat were determined for pharmacokinetic analysis. Angiotensin-converting enzyme (ACE) activity, serum ureic nitrogen (SUN), creatinine and electrolytes were measured, and blood pressure was monitored for pharmacodynamic analysis. The elimination half-lives of enalapril and enalaprilat were 0.67 and 2.76 h respectively after IV enalapril. Enalapril concentrations after PO administrations were below the limit of quantification (10 ng/ml) in all horses and enalaprilat concentrations were below the limit of quantification in 4 of the 7 horses. Maximum mean ACE inhibitions from baseline were 88.38, 3.24, 21.69, 26.11 and 30.19% for IV enalapril at 0.50 mg/kg, placebo and PO enalapril at 0.50, 1.00 and 2.00 mg/kg, respectively. Blood pressures, SUN, creatinine and electrolytes remained unchanged during the experiments.
[Mh] Termos MeSH primário: Inibidores da Enzima Conversora de Angiotensina/farmacocinética
Enalapril/farmacocinética
Enalaprilate/farmacocinética
Cavalos/metabolismo
[Mh] Termos MeSH secundário: Administração Intravenosa
Administração Oral
Inibidores da Enzima Conversora de Angiotensina/administração & dosagem
Inibidores da Enzima Conversora de Angiotensina/sangue
Animais
Pressão Sanguínea/efeitos dos fármacos
Nitrogênio da Ureia Sanguínea
Creatinina/sangue
Estudos Cross-Over
Relação Dose-Resposta a Droga
Enalapril/administração & dosagem
Enalapril/sangue
Enalaprilate/administração & dosagem
Enalaprilate/sangue
Meia-Vida
Estatísticas não Paramétricas
[Pt] Tipo de publicação:CLINICAL TRIAL; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Angiotensin-Converting Enzyme Inhibitors); 69PN84IO1A (Enalapril); AYI8EX34EU (Creatinine); GV0O7ES0R3 (Enalaprilat)
[Em] Mês de entrada:1510
[Cu] Atualização por classe:140804
[Lr] Data última revisão:
140804
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140629
[St] Status:MEDLINE


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[PMID]:24958844
[Au] Autor:Ferslew BC; Köck K; Bridges AS; Brouwer KL
[Ad] Endereço:Division of Pharmacotherapy and Experimental Therapeutics, UNC Eshelman School of Pharmacy (B.C.F., K.K., K.L.R.B.) and Department of Pathology, UNC School of Medicine (A.S.B.), University of North Carolina at Chapel Hill, Chapel Hill, North Carolina.
[Ti] Título:Role of multidrug resistance-associated protein 4 in the basolateral efflux of hepatically derived enalaprilat.
[So] Source:Drug Metab Dispos;42(9):1567-74, 2014 Sep.
[Is] ISSN:1521-009X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Hepatic uptake and efflux transporters govern the systemic and hepatic exposure of many drugs and metabolites. Enalapril is a pharmacologically inactive prodrug of enalaprilat. Following oral administration, enalapril is converted to enalaprilat in hepatocytes and undergoes translocation into the systemic circulation to exert its pharmacologic effect by inhibiting angiotensin-converting enzyme. Although the transport proteins governing hepatic uptake of enalapril and the biliary excretion of enalapril and enalaprilat are well established, it remains unknown how hepatically derived enalaprilat translocates across the basolateral membrane into the systemic circulation. In this study, the role of ATP-binding cassette transporters in the hepatic basolateral efflux of enalaprilat was investigated using membrane vesicles. ATP-dependent uptake of enalaprilat into vesicles expressing multidrug resistance-associated protein (MRP) 4 was significantly greater (∼3.8-fold) than in control vesicles. In contrast, enalaprilat was not transported to a significant extent by MRP3, and enalapril was not transported by either MRP3 or MRP4. The functional importance of MRP4 in the basolateral excretion of derived enalaprilat was evaluated using a novel basolateral efflux protocol developed in human sandwich-cultured hepatocytes. Under normal culture conditions, the mean intrinsic basolateral efflux clearance (CLint ,basolateral) of enalaprilat was 0.026 ± 0.012 µl/min; enalaprilat CLint,basolateral was significantly reduced to 0.009 ± 0.009 µl/min by pretreatment with the pan-MRP inhibitor MK-571. Results suggest that hepatically derived enalaprilat is excreted across the hepatic basolateral membrane by MRP4. Changes in MRP4-mediated basolateral efflux may alter the systemic concentrations of this active metabolite, and potentially the efficacy of enalapril.
[Mh] Termos MeSH primário: Enalaprilate/metabolismo
Fígado/metabolismo
Proteínas Associadas à Resistência a Múltiplos Medicamentos/metabolismo
[Mh] Termos MeSH secundário: Transportadores de Cassetes de Ligação de ATP/metabolismo
Transporte Biológico/fisiologia
Linhagem Celular
Enalapril/metabolismo
Células HEK293
Hepatócitos/metabolismo
Seres Humanos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (ABCC4 protein, human); 0 (Multidrug Resistance-Associated Proteins); 69PN84IO1A (Enalapril); GV0O7ES0R3 (Enalaprilat)
[Em] Mês de entrada:1503
[Cu] Atualização por classe:161019
[Lr] Data última revisão:
161019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140625
[St] Status:MEDLINE
[do] DOI:10.1124/dmd.114.057554



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