Dantrolene sodium salt

Description

Dantrolene is an inhibitor of calcium release from the sarcoplasmic reticulum (IC₅₀ = 0.3 μM). It binds to sarcoplasmic reticulum vesicles isolated from normal and malignant hyperthermia-susceptible (MHS) pigs with K_d values of 0.3 and 0.09 μM, respectively. Dantrolene reduces spontaneous calcium wave frequency and amplitude in the presence of calmodulin in isolated mouse cardiomyocytes with IC₅₀ values of 0.42 and 0.19 μM, respectively. It reduces the magnitude of electrically stimulated twitch tensions in isolated rat extensor digitorum longus and soleus muscles (IC₅₀ = 3 μg/ml) and MHS pigs (ED₅₀ = 0.85 mg/kg). Formulations containing dantrolene have been used in the treatment of malignant hyperthermia.

Chemical Properties

mp 279-280C 3415821

Uses

Skeletal muscle relaxant;Blocker of Ca2+ release

Uses

Dantrolene Sodium Salt is a skeletal muscle relaxant, which inhibits intracellular Ca 2+release from the sarcoplasmic reticulum.

Definition

ChEBI: The anhydrous sodium salt of dantrolene.

brand name

Dantrium (Procter & Gamble).

Biological Activity

Inhibits release of Ca 2+ from sarcoplasmic reticulum via inhibition of ryanodine receptor (RYR) channels. Displays selectivity for RYR1 and RYR3 over RYR2. Protective against the effects of a variety of conditions and agents, including excitatory amino acids. Skeletal muscle relaxant and neuroprotectant.

storage

Store at RT

References

1) Zhao?et al.?(2001),?Dantrolene inhibition of ryanodine receptor Ca2+ release channels. Molecular mechanism and isoform selectivity; J. Biol. Chem.,?276?13810 2) Frandsen and Schousboe (1992),?Mobilization of dantrolene-sensitive intracellular calcium pools is involved in the cytotoxicity induced by quisqualate and N-methyl-D-aspartate but not by 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionate and kainite in cultured cerebral cortical neurons; Proc. Natl. Acad. Sci. USA,?89?2590 3) Muehlschlegel and Sims (2009),?Dantrolene: mechanisms of neuroprotection and possible clinical applications in the neurointensive care unit; Neuro. Crit. Care,?10?103 4) Lu?et al.?(2014),?A calcium-dependent protease as a potential therapeutic target for Wolfram syndrome; Proc. Natl. Acad. Sci. USA,?111?E5292