The pharmacology of intracellular Ca2+-release channels

Barbara E. Ehrlich, Ed Kaftan, Svetlana Bezprozvannaya, Ilya Bezprozvanny

Research output: Contribution to journalArticlepeer-review

421 Scopus citations


Two classes of intracellular Ca2+-release channels, the ryanodine reccptor and the mositol (1,4,5)-trisphosphate (IP3) receptor, are essential for spatiotemporal Ca2+ signalling in cells. Heparin and caffeine have been widely used to study these channels. It was originally thought that caffeine acts solely as an agonist for the ryanodine receptoi and heparin acts solely as an inhibitor for the IP3 receptor. However, recent experiments indicate that these compounds have multiple effects, and are discussed in this review by Barbara Ehrlich and colleagues. In the same concentration range, caffeine activates the ryanodine receptor and inhibits the IP3 receptor, and hepaun inhibits the IP3 receptor and activates the ryanodine leceptor. More specific pharmacological tools that are suitable for studies of ryanodine and IP3 receptors are now beginning to emerge.

Original languageEnglish (US)
Pages (from-to)145-149
Number of pages5
JournalTrends in Pharmacological Sciences
Issue number5
StatePublished - May 1994

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology


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