Enrasentan improves survival, limits left ventricular remodeling, and preserves myocardial performance in hypertensive cardiac hypertrophy and dysfunction

J Cardiovasc Pharmacol. 2001 Oct;38(4):606-17. doi: 10.1097/00005344-200110000-00013.

Abstract

Evidence suggests that endothelin receptor antagonists may have therapeutic potential for the chronic treatment of heart failure. In the current study, the effects of an orally active mixed endothelin-A/endothelin-B (ETA /ETB ) receptor antagonist (enrasentan) were assessed in a model of cardiac hypertrophy and dysfunction (spontaneously hypertensive stroke prone rats) maintained on a high-salt/high-fat diet. Echocardiography was used to quantify cardiac performance and left ventricular dimensions. Enrasentan (1,200 and 2,400 parts per million in the high-salt/high-fat diet) had no significant effects on body weight and systolic blood pressure. However, increases in heart rate were not observed in the enrasentan-treated groups at 12 weeks (p < 0.05). Enrasentan-treated groups exhibited significantly improved survival (90-95% vs. 30% [control rats] at 18 weeks; p < 0.001). Enrasentan treatments also increased stroke volume (at 8, 12, and 16 weeks) and cardiac index (at 8 and 16 weeks) 33-50% and 45-63%, respectively. Enrasentan treatments reduced the relative wall thickness (14-27% at 8 and 12 weeks), ratio of left ventricular mass to body weight (20% at 12 weeks), and ratio of terminal heart weight to body weight (16-23%, p < 0.05). Finally, circulating aldosterone concentration (54-57%) and proANF fragment (33%) were reduced in enrasentan-treated groups (54-57% and 33%, respectively). Mixed ETA /ETB receptor antagonism improves cardiac performance and attenuates ventricular remodeling and premature mortality in an aggressive hypertension model.

MeSH terms

  • Aldosterone / blood
  • Animals
  • Atrial Natriuretic Factor / blood
  • Blood Pressure / drug effects
  • Blood Pressure / physiology
  • Carboxylic Acids / therapeutic use*
  • Endothelin Receptor Antagonists
  • Heart Rate / drug effects
  • Heart Rate / physiology
  • Hypertension / blood
  • Hypertension / drug therapy*
  • Hypertension / mortality
  • Hypertrophy, Left Ventricular / blood
  • Hypertrophy, Left Ventricular / drug therapy*
  • Hypertrophy, Left Ventricular / mortality
  • Indans / therapeutic use*
  • Male
  • Myocardium / metabolism
  • Protein Precursors / blood
  • Rats
  • Rats, Inbred SHR
  • Survival Rate
  • Ventricular Remodeling / drug effects*
  • Ventricular Remodeling / physiology

Substances

  • Carboxylic Acids
  • Endothelin Receptor Antagonists
  • Indans
  • Protein Precursors
  • Aldosterone
  • Atrial Natriuretic Factor
  • enrasentan