Comparative study of the block of Vmax by aprindine and quinidine in the guinea-pig heart muscle

Eur J Pharmacol. 1988 Aug 24;153(2-3):285-8. doi: 10.1016/0014-2999(88)90616-4.

Abstract

The depression of Vmax of the action potential in guinea-pig ventricular muscle by aprindine and quanidine was compared. Aprindine caused a more pronounced rate-dependent block (Kd = 10(-6) M at 3.3 Hz) than did quinidine (Kd = 1.6 X 10(-5) M at 3.3 Hz). Aprindine shifted the relationship between Vmax and resting potential to a more negative potential (mean 9.2 mV: 10 microM) than did quinidine (mean 5.7 mV: 10 microM). In addition, aprindine caused a more pronounced resting block (Kd = 1.3 X 10(-5) M) than quinidine (Kd = 8.6 X 10(-5) M). It is concluded that aprindine has a higher affinity for activated and/or inactivated and resting state channels than quinidine, making channels unavailable for conduction upon activation.

Publication types

  • Comparative Study

MeSH terms

  • Action Potentials / drug effects
  • Animals
  • Aprindine / pharmacology*
  • Electric Stimulation
  • Guinea Pigs
  • In Vitro Techniques
  • Indenes / pharmacology*
  • Kinetics
  • Membrane Potentials / drug effects
  • Papillary Muscles / drug effects*
  • Papillary Muscles / physiology
  • Quinidine / pharmacology*
  • Sodium Channels / drug effects
  • Sodium Channels / metabolism

Substances

  • Indenes
  • Sodium Channels
  • Aprindine
  • Quinidine