Inhibition of Na+/Ca2+ exchange by hexapeptide FRCRSFa in rat ventricular myocytes

Acta Pharmacol Sin. 2002 Jun;23(6):529-33.

Abstract

Aim: To study the effect of Phe-Arg-Cys-Arg-Ser-Phe-CONH2 (FRCRSFa) on Na+/Ca2+ exchange and its specificity in rat ventricular myocytes.

Methods: Na+/Ca2+ exchange current (INa+/Ca2+) and other currents were measured using whole-cell voltage clamp technique.

Results: A concentration-dependent inhibition of hexapeptide FRCRSFa on Na +/Ca2+ exchange was observed in rat ventricular myocytes. IC50 of inward and outward INa+/Ca2+ were 2 and 4 micromol/L, respectively. FRCRSFa 5 micromol/L did not affect L-type Ca2+ current, voltage-gated Na+ current, transient outward K+ current, and inward rectifier K+ current.

Conclusion: These data indicate that FRCRSFa is an available inhibitor of Na+/Ca2+ exchange with relative selectivity and m ay be valuable for studies of the Na+/Ca2+ exchange in cardiac myocytes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Separation
  • Depression, Chemical
  • Heart Ventricles / cytology
  • Myocytes, Cardiac / metabolism*
  • Oligopeptides / pharmacology*
  • Peptides / pharmacology
  • Rats
  • Rats, Wistar
  • Sodium-Calcium Exchanger / antagonists & inhibitors*

Substances

  • Oligopeptides
  • Peptides
  • Sodium-Calcium Exchanger
  • phenylalanyl-arginyl-cysteinyl-arginyl-seryl-phenylalaninamide