Suramin increases the efficacy of ATP to activate an inward current in myenteric neurons from guinea-pig ileum

Eur J Pharmacol. 1993 Nov 30;250(1):141-5. doi: 10.1016/0014-2999(93)90631-q.

Abstract

Previous reports have indicated that suramin antagonizes, in a competitive manner, the actions of adenosine 5'-triphosphate (ATP) mediated by P2 purinoceptors. In neurons from the myenteric plexus, however, suramin has different effects on an ATP-activated conductance. During whole-cell recordings, ATP (3-1000 microM) evoked a rapidly desensitizing inward current in a concentration-dependent manner. The amplitude of the ATP-activated current was increased, in a reversible manner, when suramin was applied previous to or during ATP stimulation. This effect was increased by raising the suramin concentration. Higher concentrations of suramin were required for higher concentrations of ATP; the EC50 values of suramin were 5 +/- 1.1 microM and 143 +/- 48 nM when ATP concentrations of 30 and 10 microM were used. No change in the holding current was observed with suramin alone. These observations suggest that a different subtype of P2 purinoceptors could be expressed in the myenteric neurons.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Triphosphate / pharmacology*
  • Animals
  • Cells, Cultured
  • Dose-Response Relationship, Drug
  • Electrophysiology
  • Female
  • Guinea Pigs
  • Ileum / innervation*
  • Male
  • Myenteric Plexus / cytology
  • Myenteric Plexus / drug effects*
  • Myenteric Plexus / physiology
  • Neurons / drug effects
  • Receptors, Purinergic / drug effects*
  • Receptors, Purinergic / metabolism
  • Suramin / pharmacology*

Substances

  • Receptors, Purinergic
  • Suramin
  • Adenosine Triphosphate