Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyte glutathione reductase. K_i and IC₅₀ values are 111.6 μM and 52.3 μM, respectively. Dantrolene is a ryanodine receptor antagonist and Ca²⁺ signaling stabilizer. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome^[4][5].

Dantrolene interferes with calcium release from the sarcoplasmic reticulum and thus to inhibit excitation--contraction coupling.
Dantrolene acts directly on the RYR1 to reduce the extent of channel activation by calmodulin (CaM) and thereby decreases the Ca²⁺ sensitivity of channel activation.
Dantrolene inhibits abnormal Ca²⁺ release from the sarcoplasmic reticulum.
Dantrolene depresses excitation-contraction coupling in muscle fibers by inhibiting calcium release from the sarcoplasmic reticulum.
Dantrolene also shows calcium channel blocker effect in the smooth muscle membrane as well as antioxidative and cytoprotective properties.
Dantrolene affects the membrane calcium channel of smooth muscle cells and inhibits calcium influx.
Dantrolene is a skeletal muscle-specific muscle relaxant that works on the cardiac muscle. Dantrolene (0.3 μM) binds to domain 601-620 of RyR2 and corrects defective inter-domain interaction within RyR2 in failing hearts. This in turn inhibits spontaneous Ca²⁺+ leak/Ca²⁺ sparks, and improves cardiomyocyte function in failing hearts^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Dantrolene is neuroprotective in Huntington's disease transgenic mouse model^[5].
Feeding dantrolene (5 mg/kg) twice a week to YAC128 mice between 2 months and 11.5 months of age resulted in significantly improved performance in the beam-walking and gait-walking assays^[5].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Dantrolene is neuroprotective in Huntington's disease transgenic mouse model^[5].
Feeding dantrolene (5 mg/kg) twice a week to YAC128 mice between 2 months and 11.5 months of age resulted in significantly improved performance in the beam-walking and gait-walking assays^[5].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . W J Meyler, et al. The effect of dantrolene sodium on rat skeletal muscle in relation to the plasma concentration. Eur J Pharmacol. 1979 Feb 1;53(4):335-42.  [Content Brief]

  . F Zhao, et al. Dantrolene inhibition of ryanodine receptor Ca2+ release channels. Molecular mechanism and isoform selectivity. J Biol Chem. 2001 Apr 27;276(17):13810-6.  [Content Brief]

  . Murat Sentürk, et al. Dantrolene inhibits human erythrocyte glutathione reductase. Biol Pharm Bull. 2008 Nov;31(11):2036-9.  [Content Brief]

  [4]. Shigeki Kobayashi, et al. Dantrolene, a therapeutic agent for malignant hyperthermia, markedly improves the function of failing cardiomyocytes by stabilizing interdomain interactions within the ryanodine receptor. J Am Coll Cardiol. 2009 May 26;53(21):199  [Content Brief]

  [5]. Xi Chen, et al. Dantrolene is neuroprotective in Huntington's disease transgenic mouse model. Mol Neurodegener. 2011 Nov 25;6:81.  [Content Brief]