Caffeine-induced inhibition of inositol(1,4,5)-trisphosphate-gated calcium channels from cerebellum

Ilya Bezprozvanny, Svetlana Bezprozvannaya, Barbara E. Ehrlich

Research output: Contribution to journalArticlepeer-review

85 Scopus citations


Effects of the xanthine drug caffeine on inositol (1,4,5)-trisphosphate (InsP3)-gated calcium (Ca) channels from canine cerebellum were studied using single channels incorporated into planar lipid bilayers. Caffeine, used widely as an agonist of ryanodine receptors, inhibited the activity of InsP3-gated Ca channels in a noncooperative fashion with half-inhibition at 1.64 mM caffeine. The frequency of channel openings was decreased more than threefold after addition of 5 mM caffeine; there was only a small effect on mean open time of the channels, and the single channel conductance was unchanged. Increased InsP3 concentration overcame the inhibitory action of caffeine, but caffeine did not reduce specific [3H]InsP3 binding to the receptor. The inhibitory action of caffeine on InsP3 receptors suggests that the action of caffeine on the intracellular Ca pool must be interpreted with caution when both ryanodine receptors and InsP3 receptors are present in the cell.

Original languageEnglish (US)
Pages (from-to)97-103
Number of pages7
JournalMolecular biology of the cell
Issue number1
StatePublished - Jan 1994

ASJC Scopus subject areas

  • Molecular Biology
  • Cell Biology


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