Dantrolene mechanism


Dantrolene is a hydrophobic, hydantoin derivative that suppresses the rate and amount of Calcium ions (Ca2+) released from the sarcoplasmic reticulum. Specifically, dantrolene inhibits RyR1-dependent cellular Ca2+ fluxes in skeletal muscle.   It is unclear whether or not the significant increases in malignant hyperthermia result from the release of Ca2+ from the sarcoplasmic reticulum or from the re-entry of Ca2+ from extracellular sources, but it has been shown that dantrolene acts on the RyR1 channel in skeletal muscle to affect Ca2+ fluxes.


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Emily Knipper, MD