Name | dantrolene |
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Synonyms |
Dantrium
1-[5-(4-nitro-phenyl)-furan-2-ylmethyleneamino]-imidazolidine-2,4-dione 1-[(E)-[5-(4-nitrophenyl)furan-2-yl]methylideneamino]imidazolidine-2,4-dione Dantroleno [INN-Spanish] Dantrolenum [INN-Latin] UNII-F64QU97QCR danthrolene Dantrium Intravenous Dantrolenum 1-[((5-(4-nitrophenyl)-2-furanyl)methylene)amino]-2,4-imidazolidinedione Dantroleno |
Description | Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyte glutathione reductase. Ki 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[1][2][3][4][5]. |
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Related Catalog | |
In Vitro | Dantrolene interferes with calcium release from the sarcoplasmic reticulum and thus to inhibit excitation--contraction coupling[1]. 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[2]. Dantrolene inhibits abnormal Ca2+ release from the sarcoplasmic reticulum[3]. Dantrolene depresses excitation-contraction coupling in muscle fibers by inhibiting calcium release from the sarcoplasmic reticulum[3]. Dantrolene also shows calcium channel blocker effect in the smooth muscle membrane as well as antioxidative and cytoprotective properties[3]. Dantrolene affects the membrane calcium channel of smooth muscle cells and inhibits calcium influx[3]. 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]. |
In Vivo | 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]. Animal Model: YAC128 transgenic mice (FVBN/NJ background strain) and WT mice[5] Dosage: 5 mg/kg Administration: Fed orally twice per week from 2 to 11.5 months of age, followed by a washout period of 2 months (13.5 months of age) Result: Resulted in significantly improved performance in the beam-walking and gait-walking assays. |
References |
Density | 1.57 g/cm3 |
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Boiling Point | 175-177ºC |
Melting Point | 279-280°C (lit.) |
Molecular Formula | C14H10N4O5 |
Molecular Weight | 314.25300 |
Exact Mass | 314.06500 |
PSA | 120.73000 |
LogP | 2.53040 |
Index of Refraction | 1.715 |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
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Hazard Codes | Xi |
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RIDADR | NONH for all modes of transport |