Key result
Decreasing free calcium concentration with ≥10 mM EGTA increased specific [3H]dantrolene binding to the cardiac ryanodine receptor (RyR2) by approximately 2-fold.
Absolute Event Rate: 2.21% vs 1.13%
p-value: p=< 10^-5
Dantrolene binds to a conformationally sensitive site on the cardiac ryanodine receptor (RyR2), highlighting a potential therapeutic target for diseases with dysfunctional intracellular Ca2+ release.
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Questions dantrolene effects on cardiac RyR2; leaves open isoform-selective targeting for heart failure therapies.
Paul-Pletzer et al. (2005) studied this question. Dantrolene and EGTA vs. Dantrolene without EGTA was evaluated on [3H]Dantrolene binding to RyR2 (pmol/mg of protein) (p=< 10^-5). Decreasing free calcium concentration with ≥10 mM EGTA increased specific [3H]dantrolene binding to the cardiac ryanodine receptor (RyR2) by approximately 2-fold.
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