[3H]α,β-methylene ATP binding to P2X purinoceptor is unaffected by volatile anaesthetics

Eiji Masaki, K. Yamazaki, S. Hori, M. Kawamura

Research output: Contribution to journalArticlepeer-review

1 Citation (Scopus)


Background and objective: The P2X receptor is responsible for fast excitatory neurotransmission in the central nervous system. This receptor is suggested as one of the targets of volatile anaesthetics. The study was undertaken to examine the site of action of volatile anaesthetics, especially for P2X purinoceptor-mediated neurotransmission. Methods: The effect of sevoflurane and isoflurane on [3H]α,β-methylene ATP binding was investigated in rat crude synaptic membranes. The crude synaptic membranes were prepared from Sprague-Dawley rat brains by centrifugation and then incubated with volatile anaesthetics or P2 receptor antagonists. Results: [3H]α,β-methylene ATP binding was unchanged by either sevoflurane or isoflurane at clinically relevant concentrations. Suramin, a P2 antagonist, significantly (P < 0.05) decreased the binding of [ 3H]α,β-methylene ATP in a dose-dependent manner (68.7 ± 14.7% at 10 μmol, 49.5 ± 6.4% at 50 μmol, 24.3 ± 5.7% at 100 μmol, n = 10, mean ± SD), whereas pyridoxal-phosphate-6-azophenyl-2′,4′-disulphonic acid (PPADS), another P2 antagonist, did not affect the binding. Conclusions: The suppressive effect of volatile anaesthetics on ATP-mediated excitatory synaptic transmission could be one site of action. However, the blockade of ATP binding to P2X receptors is not a mechanism of action of volatile anaesthetics.

Original languageEnglish
Pages (from-to)221-225
Number of pages5
JournalEuropean Journal of Anaesthesiology
Issue number3
Publication statusPublished - 2004 Mar 1


  • Adenine Nucleotides, adenosine triphosphate
  • Anaesthetics General, anaesthetics inhalation, isoflurane, sevoflurane
  • Membrane Transport Proteins, ion channels
  • Neurotransmitters

ASJC Scopus subject areas

  • Anesthesiology and Pain Medicine


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