Dantrolene (F368) 是一种肌肉松弛剂，非竞争性地抑制人红细胞谷胱甘肽还原酶 (glutathione reductase)，Ki和IC50值分别为 111.6 μM 和 52.3 μM。 Dantrolene 是一种兰尼碱受体拮抗剂和 Ca2+信号稳定剂。Dantrolene 可用于肌肉痉挛、恶性高热、亨廷顿病和其他神经阻滞剂恶性综合征的研究。
| 生物活性 | Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyteglutathione reductase.KiandIC50values 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]. |
体外研究
(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].
|
体内研究
(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. |
|
| Clinical Trial | |
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 中文名称 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
| 溶解性数据 | In Vitro: DMSO : ≥ 20 mg/mL(63.64 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.1822 mL | 15.9109 mL | 31.8218 mL | | 5 mM | 0.6364 mL | 3.1822 mL | 6.3644 mL | | 10 mM | 0.3182 mL | 1.5911 mL | 3.1822 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 1. Dantrolene is suspended in 50 μL of PBS with 2% corn flour[5].
|
m.cnreagent.com