Effects of the vasopeptidase inhibitor omapatrilat on peri- and postmyocardial infarction in Zucker lean rats

Can J Cardiol. 2005 Mar;21(3):291-7.

Abstract

Background: The vasopeptidase inhibitor omapatrilat improves insulin sensitivity and survival following myocardial infarction (MI). It also improves left ventricular (LV) remodelling following MI and reduces MI size.

Objectives: To determine whether improvement in LV remodelling and function is accompanied by a reduction in fetal gene expression of the contractile apparatus, and whether reduction in MI size is accompanied by an increase in the expression of the glucose transporter GLUT-4.

Methods: Eighty-nine rats were pretreated for seven days with omapatrilat 20 mg/kg/day and 91 rats were left untreated. MI was induced in 180 Zucker lean male rats by ligating the left anterior descending coronary artery, and omapatrilat was given for another 38 days in the survivors. After 30 days, echocardiography was performed. At 38 days, hemodynamic measurements were performed, the rats were sacrificed and morphological measurements were done. Using quantitative reverse transcriptase-polymerase chain reaction, gene expression was measured in the LV using transcript levels.

Results: Treatment with omapatrilat resulted in improved early (24 h) and late (38 days) survival following MI (50% to 67%, P=0.023, and 44% to 59%, P=0.045, respectively). Omapatrilat treatment reduced MI size and resulted in beneficial ventricular remodelling as reflected by a reduction in cardiac dimensions by echocardiography, and LV and right ventricular hypertrophy, which resulted in borderline hemodynamic improvement. A large MI resulted in an increased expression of beta-myosin heavy chain, alpha-skeletal actin and atrial natriuretic peptide, and a decreased expression of GLUT-4. Omapatrilat treatment did not modify the expression of these genes.

Conclusions: The results suggest that the vasopeptidase inhibitor omapatrilat does not modify fetal gene expression of the contractile apparatus or the expression of GLUT-4 despite reducing cardiac hypertrophy and MI size.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Atrial Natriuretic Factor / analysis
  • Atrial Natriuretic Factor / drug effects
  • Atrial Natriuretic Factor / genetics
  • Disease Models, Animal*
  • Drug Evaluation, Preclinical
  • Echocardiography
  • Gene Expression Regulation / drug effects
  • Glucose Transporter Type 4
  • Heart Ventricles / chemistry
  • Hypertrophy, Left Ventricular / etiology
  • Hypertrophy, Right Ventricular / etiology
  • Ligation
  • Male
  • Monosaccharide Transport Proteins / analysis
  • Monosaccharide Transport Proteins / drug effects
  • Monosaccharide Transport Proteins / genetics
  • Muscle Proteins / analysis
  • Muscle Proteins / drug effects
  • Muscle Proteins / genetics
  • Myocardial Infarction / complications
  • Myocardial Infarction / drug therapy*
  • Myocardial Infarction / mortality
  • Myocardial Infarction / physiopathology
  • Protease Inhibitors / pharmacology
  • Protease Inhibitors / therapeutic use*
  • Pyridines / pharmacology
  • Pyridines / therapeutic use*
  • Random Allocation
  • Rats
  • Rats, Zucker
  • Reverse Transcriptase Polymerase Chain Reaction
  • Survival Rate
  • Thiazepines / pharmacology
  • Thiazepines / therapeutic use*
  • Ventricular Function, Left / drug effects
  • Ventricular Myosins / analysis
  • Ventricular Myosins / drug effects
  • Ventricular Myosins / genetics
  • Ventricular Remodeling / drug effects

Substances

  • Glucose Transporter Type 4
  • Monosaccharide Transport Proteins
  • Muscle Proteins
  • Protease Inhibitors
  • Pyridines
  • Slc2a4 protein, rat
  • Thiazepines
  • omapatrilat
  • Atrial Natriuretic Factor
  • Ventricular Myosins