Key result
Dantrolene, a ryanodine receptor antagonist, demonstrates cytoprotective effects against cell damage in various models of stress and disease by inhibiting abnormal intracellular calcium release.
This review highlights the potential of dantrolene as a cytoprotective agent across various disease models characterized by intracellular calcium dysregulation.
Supports dantrolene investigation for cytoprotection in calcium dysregulation disorders; leaves open clinical translation pending trials.
Calcium, as a second messenger, has an important role in a variety of cellular functions. However, disruption of intracellular calcium homeostasis leads to cytotoxicity and cell death. Excessive calcium release from intracellular stores, via the calcium channel ryanodine receptor, contributes to cell damage. Dysfunction of calcium homeostasis is established in tissue culture and animal models of ischemia, hypoxia, seizure, trauma, anesthesia, and neurodegenerative diseases. Dantrolene, the primary drug to treat malignant hyperthermia, is a ryanodine receptor antagonist. Dantrolene inhibits abnormal calcium release from the sarco-endoplasmic reticulum, which is the primary intracellular calcium store. Dantrolene has been investigated widely for its possible cytoprotective effects against cell damage in different tissue culture or animal models of diseases involving cytotoxicity induced by disruption of intracellular calcium homeostasis in pathogenesis. In this review, we summarize the role of the disruption of intracellular calcium homeostasis on cell death, the pharmacologic and pharmacokinetic features of dantrolene, and the cytoprotective effects and potential application of dantrolene for the inhibition of cell damage in a wide variety of models of stress and disease.
No takes yet. Share an insight, caveat, or question.
Inan et al. (2010) conducted a review in Cytotoxicity and cell damage induced by disruption of intracellular calcium homeostasis. Dantrolene was evaluated. Dantrolene, a ryanodine receptor antagonist, demonstrates cytoprotective effects against cell damage in various models of stress and disease by inhibiting abnormal intracellular calcium release.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: