E-1020, a water soluble imidazopyridine, has direct effects on Ca(2+)-dependent force and ATP hydrolysis of canine and bovine cardiac myofilaments

Mol Cell Biochem. 1996 Jul-Aug:160-161:33-9. doi: 10.1007/BF00240028.

Abstract

E-1020 is a cardiotonic agent that acts as a cyclic-AMP phosphodiesterase inhibitor but also may have actions which alter myofilament response to Ca2+. To identify direct actions of E-1020 on cardiac contractile proteins, effects of E-1020 on myofibrillar Ca2+ dependent MgATPase and force generation in chemically skinned fiber bundles were measured. In bovine cardiac myofibrils, E-1020 (100 microM) significantly increased myofilament Ca2+ sensitivity and Ca(2+)-dependent ATPase activity at submaximal pCa values. At pCa 6.75, E-1020 significantly increased ATPase activity in bovine (10-100 microM) and canine (1-100 microM) cardiac myofibrils but had no effect on rat cardiac myofibrils. Moreover, in one population of canine ventricular fiber bundles, E-1020 (0.01-10 microM) significantly increased isometric tension at pCa 6.5 and 6.0, whereas in another population of bundles E-1020 had no effect on tension. In no case was resting (pCa 8.0) or maximal tension (pCa 4.5) increased by E-1020. Measurements of Ca2+ binding to canine ventricular skinned fiber preparations demonstrated that E-1020 does not alter the affinity of myofilament troponin C for Ca2+. We conclude that part of the mechanism by which E-1020 acts as an inotropic agent may involve alterations in the responsiveness of contractile proteins to Ca2+. The lack of effect of E-1020 on some preparations may be dependent on isoform populations of myofilament proteins.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Actin Cytoskeleton / drug effects*
  • Actin Cytoskeleton / metabolism
  • Adenosine Triphosphate / metabolism*
  • Animals
  • Calcium / metabolism*
  • Cardiotonic Agents / pharmacology*
  • Cattle
  • Dogs
  • Hydrolysis
  • Imidazoles / pharmacology*
  • Isometric Contraction
  • Myocardium / metabolism*
  • Pyridones / pharmacology*
  • Rats

Substances

  • Cardiotonic Agents
  • Imidazoles
  • Pyridones
  • olprinone
  • Adenosine Triphosphate
  • Calcium