Suramin--a powerful inhibitor of neural ecto-diadenosine polyphosphate hydrolase

Br J Pharmacol. 1996 Sep;119(1):1-2. doi: 10.1111/j.1476-5381.1996.tb15668.x.

Abstract

The neural ecto-diadenosine polyphosphate hydrolase (ecto-ApnAase) from plasma membranes of Torpedo synaptic terminals is inhibited by suramin. This study was carried out by discontinuous h.p.l.c. and continuous fluorometric methods. The concentration-dependence studies showed a non-competitive mechanism for suramin in the Dixon plot, with a Ki value of 1.79 +/- 0.03 microM with respect to epsilon-(Ap3A) as the substrate and 1.69 +/- 0.05 microM and 1.86 +/- 0.06 microM for epsilon-(Ap4A) and epsilon-(Ap5A) respectively. These results indicate that suramin could be a base compound inhibiting ecto-ApnAase and providing an alternative way of studying the pharmacology of diadenosine polyphosphate receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acid Anhydride Hydrolases / analysis*
  • Acid Anhydride Hydrolases / antagonists & inhibitors*
  • Acid Anhydride Hydrolases / metabolism
  • Animals
  • Cell Membrane / drug effects
  • Cell Membrane / metabolism
  • Chromatography, High Pressure Liquid
  • Dose-Response Relationship, Drug
  • Electric Organ / drug effects
  • Electric Organ / metabolism
  • Enzyme Inhibitors / pharmacology*
  • Fluorometry
  • Kinetics
  • Suramin / pharmacology*
  • Synapses / drug effects
  • Synapses / enzymology*
  • Torpedo / metabolism

Substances

  • Enzyme Inhibitors
  • Suramin
  • Acid Anhydride Hydrolases
  • diadenosine polyphosphate hydrolase