Protective effect of HOE642, a selective blocker of Na+-H+ exchange, against the development of rigor contracture in rat ventricular myocytes

Exp Physiol. 2000 Jan;85(1):17-25.

Abstract

The objective of this study was to investigate the effect of Na+-H+ exchange (NHE) and HCO3--Na+ symport inhibition on the development of rigor contracture. Freshly isolated adult rat cardiomyocytes were subjected to 60 min metabolic inhibition (MI) and 5 min re-energization (Rx). The effects of perfusion of HCO3- or HCO3--free buffer with or without the NHE inhibitor HOE642 (7 microM) were investigated during MI and Rx. In HCO3--free conditions, HOE642 reduced the percentage of cells developing rigor during MI from 79 +/- 1% to 40 +/- 4% (P < 0.001) without modifying the time at which rigor appeared. This resulted in a 30% reduction of hypercontracture during Rx (P < 0.01). The presence of HCO3- abolished the protective effect of HOE642 against rigor. Cells that had developed rigor underwent hypercontracture during Rx independently of treatment allocation. Ratiofluorescence measurement demonstrated that the rise in cytosolic Ca2+ (fura-2) occurred only after the onset of rigor, and was not influenced by HOE642. NHE inhibition did not modify Na+ rise (SBFI) during MI, but exaggerated the initial fall of intracellular pH (BCEFC). In conclusion, HOE642 has a protective effect against rigor during energy deprivation, but only when HCO3--dependent transporters are inhibited. This effect is independent of changes in cytosolic Na+ or Ca2+ concentrations.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Bicarbonates / metabolism
  • Calcium / metabolism
  • Energy Metabolism / physiology
  • Enzyme Inhibitors / pharmacology*
  • Guanidines / pharmacology*
  • Heart / drug effects*
  • Heart Ventricles / cytology
  • Heart Ventricles / drug effects
  • Heart Ventricles / enzymology
  • Hydrogen-Ion Concentration
  • In Vitro Techniques
  • L-Lactate Dehydrogenase / metabolism
  • Male
  • Myocardial Contraction / drug effects*
  • Myocardium / cytology*
  • Myocardium / enzymology
  • Perfusion
  • Rats
  • Rats, Sprague-Dawley
  • Rigor Mortis / enzymology
  • Rigor Mortis / prevention & control*
  • Sodium / metabolism
  • Sodium-Hydrogen Exchangers / antagonists & inhibitors*
  • Sulfones / pharmacology*

Substances

  • Bicarbonates
  • Enzyme Inhibitors
  • Guanidines
  • Sodium-Hydrogen Exchangers
  • Sulfones
  • cariporide
  • Sodium
  • L-Lactate Dehydrogenase
  • Calcium