Key result
Gallopamil inhibits ryanodine binding to its low affinity sites and modulates the cooperativity of ryanodine binding or the transition to a slow dissociation state in rat heart sarcoplasmic reticulum.
Population
Sarcoplasmic reticulum fraction obtained from rat hearts
Design
Preclinical
Authors
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Hypothesis-generating for gallopamil effects on cardiac SR calcium release in rats; human relevance and therapeutic translation remain untested.
Gallopamil inhibits ryanodine binding to its low affinity sites and modulates cooperativity, providing a molecular mechanism for its effects on the sarcoplasmic reticulum calcium release channel.
Zucchi et al. (1995) studied this question. Gallopamil was evaluated on Interaction with cardiac ryanodine receptors (binding and dissociation). Gallopamil inhibits ryanodine binding to its low affinity sites and modulates the cooperativity of ryanodine binding or the transition to a slow dissociation state in rat heart sarcoplasmic reticulum.
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