The skeletal muscle relaxant dantrolene inhibits the release of Ca2+ from the sarcoplasmic reticulum during excitation-contraction coupling and suppresses the uncontrolled Ca2+ release that underlies the skeletal muscle pharmacogenetic disorder malignant hyperthermia; however, the molecular mechanism by which dantrolene selectively affects skeletal muscle Ca2+ regulation remains to be defined. ...

Rapid and efficient cooling is the most important therapeutic objective in patients with heat stroke (HS). This article reviews the mechanism of action and rationale for the use of dantrolene as a potential supportive cooling method in the treatment of HS. Relevant studies were included to support discussion of the role of dantrolene for the treatment of HS. In some studies dantrolene was shown...

Maxwell JT, Domeier TL, Blatter LA. Dantrolene prevents arrhythmogenic Ca release in heart failure. Am J Physiol Heart Circ Physiol 302: H953–H963, 2012. First published December 16, 2011; doi:10.1152/ajpheart.00936.2011.—In heart failure (HF), arrhythmogenic Ca release and chronic Ca depletion of the sarcoplasmic reticulum (SR) arise due to altered function of the ryanodine receptor (RyR) SR C...

Kindling phenomenon (an experimental model of acquired epilepsy) and long-term potentiation (LTP) have many features in common. LTP is associated with an increase in intracellular Ca(2+) concentration where intracellular Ca(2+) stores play an important role. Dantrolene has an inhibitory action against Ca(2+) release from intracellular Ca(2+) stores. This substance has been reported to inhibit t...

Purpose: To examine the use of intravenous dantrolene in hospitalized patients. Materials and Methods: Medical Records of patients treated with intravenous dantrolene between 2007 and 2012 at 6 teaching hospitals were reviewed. Temperature, muscle rigidity, creatine kinase levels, and mortality were assessed in association with dantrolene use. Results: Twenty-five patients received intravenous ...

PURPOSE A virtual screening study has suggested that the skeletal muscle relaxant, dantrolene, and the antiemetic drug, ondansetron, may act as inhibitors of the enzyme acetylcholinesterase (AChE). Based on this proposal, the current study examines the AChE inhibitory properties of these drugs. METHODS AND FINDINGS Using AChE from human erythrocytes as enzyme source, it is shown that dantrole...

We investigated the actions of dantrolene Ca(2+)-induced on Ca(2+)-release (CICR) evoked by action potentials in cultured rat sensory neurons. The effect of dantrolene on action potential after-depolarization and voltage-activated calcium currents was studied in cultured neonatal rat dorsal root ganglion cells (DRG) using the whole-cell patch-clamp technique. Depolarizing current injection evok...

As an inhibitor of Ca(2+) release through ryanodine receptor (RYR) channels, the skeletal muscle relaxant dantrolene has proven to be both a valuable experimental probe of intracellular Ca(2+) signaling and a lifesaving treatment for the pharmacogenetic disorder malignant hyperthermia. However, the molecular basis and specificity of the actions of dantrolene on RYR channels have remained in que...

Introduction: Dantrolene is a muscle relaxant used to treat malignant hyperthermia as well as muscle spasms in spinal cord injury patients. It is known to cause a decrease in skeletal muscle strength in humans, and inhibit diaphragm muscle strength in hamsters. There is at least one other case report of dantrolene leading to respiratory failure in a spinal cord injury patient. Here we present a...