Activation of the calcium release channel (ryanodine receptor) by heparin and other polyanions is calcium dependent

Ilya B. Bezprozvanny, Karol Ondrias, Edward Kaftan, Detcho A. Stoyanovsky, Barbara E. Ehrlich

Research output: Contribution to journalArticle

64 Citations (Scopus)

Abstract

Heparin has been used as a potent competitive inhibitor of inositol 1,4,5-trisphosphate (IP 3)-binding to IP 3 receptors and to block IP 3-gated calcium channels in bilayer experiments. In contrast to the effect on the IP 3-gated channel, heparin (0.1-1 μg/ml) opened the Ca release channel (ryanodine receptor). Other polyanions such as pentosan polysulfate and polyvinyl sulfate also activated the Ca release channel. The effect of polyanions on the Ca release channel was Ca dependent. Polyanion addition activated the Ca release channel when free Ca was >80 nM, but was ineffective when free Ca was <20 nM. The level of channel activation could be altered by manipulating the free Ca concentration. These results suggest that the polyanions act by increasing the local concentration of Ca near regulatory sites on the channel complex. As most cells have both types of intracellular channels, the opposite effects of the polyanions on the two channel types suggests that addition of polyanions to intact cells may produce multiple effects.

Original languageEnglish (US)
Pages (from-to)347-352
Number of pages6
JournalMolecular Biology of the Cell
Volume4
Issue number3
StatePublished - 1993

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Ryanodine Receptor Calcium Release Channel
Heparin
Calcium
Pentosan Sulfuric Polyester
Inositol 1,4,5-Trisphosphate
Calcium Channels
polyanions

ASJC Scopus subject areas

  • Molecular Biology
  • Genetics
  • Cell Biology

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Activation of the calcium release channel (ryanodine receptor) by heparin and other polyanions is calcium dependent. / Bezprozvanny, Ilya B.; Ondrias, Karol; Kaftan, Edward; Stoyanovsky, Detcho A.; Ehrlich, Barbara E.

In: Molecular Biology of the Cell, Vol. 4, No. 3, 1993, p. 347-352.

Research output: Contribution to journalArticle

Bezprozvanny, Ilya B. ; Ondrias, Karol ; Kaftan, Edward ; Stoyanovsky, Detcho A. ; Ehrlich, Barbara E. / Activation of the calcium release channel (ryanodine receptor) by heparin and other polyanions is calcium dependent. In: Molecular Biology of the Cell. 1993 ; Vol. 4, No. 3. pp. 347-352.
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