Pflügers Archiv

, Volume 418, Issue 3, pp 214–219

Effects of ATP antagonists on purinoceptor-operated inward currents in rat phaeochromocytoma cells

  • Ken Nakazawa
  • Kazuhide Inoue
  • Kannosuke Fujimori
  • Akira Takanaka
Excitable Tissues and Central Nervous Physiology


The effects of suramin, reactive blue 2 (RB2) and d-tubocurarine (d-TC) were investigated electrophysiologically to elucidate the mechanisms underlying their antagonism of P2 purinoceptor-mediated responses. All three compounds inhibited an adenosine triphosphate (ATP)-activated inward current in rat phaeochromocytoma PC12 cells in a concentration-dependent manner. The order of potency was RB2 > suramin > d-TC. The inhibition induced by suramin or RB2 was reversible, whereas that induced by d-TC was not reversed after a 5-min rinse. The inactivation of the ATP-activated current was accelerated by d-TC but not by suramin or RB2. RB2 administered simultaneously with ATP exerted much weaker inhibition compared to that induced by prior administration, suggesting that RB2 is a slowly acting antagonist. This was not observed for suramin or d-TC. Suramin and RB2 caused a parallel shift in the concentration/response curve for the ATP-activated current. With d-TC the maximal response of ATP was decreased but the concentration producing half-maximal response was unchanged. The voltage dependency of the ATP-activated current showed less inward rectification in the presence of d-TC. Suramin or RB2 did not affect the voltage dependency. These results suggest that suramin and RB2 reversibly block binding of ATP to receptors, whereas d-TC blocks ion permeability through the ATP-activated channel.

Key words

Adenosine triphosphate Purinoceptor Antagonist Non-specific cation channel Phaeochromocytoma cells 


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Copyright information

© Springer-Verlag 1991

Authors and Affiliations

  • Ken Nakazawa
    • 1
  • Kazuhide Inoue
    • 1
  • Kannosuke Fujimori
    • 1
  • Akira Takanaka
    • 1
  1. 1.Division of PharmacologyNational Institute of Hygienic SciencesTokyoJapan

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