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Dantrolene

CAS No. : 7261-97-4

MCE 站：Dantrolene

产品活性：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)，K_i 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。

研究领域：Others

作用靶点：Others

In Vitro: Dantrolene interferes with calcium release from the sarcoplasmic reticulum ａnd thus to inhibit excitation－－contraction coupling.
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.
Dantrolene inhibits abnormal Ca²⁺ release from the sarcoplasmic reticulum.
Dantrolene depresses excitation-contraction coupling in muscle fibers by inhibiting calcium release from the sarcoplasmic reticulum.
Dantrolene also shows calcium channel blocker effect in the smooth muscle membrane as well as antioxidative ａnd cytoprotective properties.
Dantrolene affects the membrane calcium channel of smooth muscle cells ａnd inhibits calcium influx.
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.

In Vivo: Dantrolene is neuroprotective in Huntington＇s disease transgenic mouse model.
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.

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