Dantrolene sodium  (Synonyms: 丹曲洛林钠盐; F 440)

Dantrolene sodium is an orally active, non-competitive glutathione reductase inhibitor with a K_i of 111.6 μM and an IC₅₀ of 52.3 μM. Dantrolene sodium is also a calcium channel protein inhibitor. Dantrolene sodium inhibits the release of Ca²⁺ from RyR1 and RyR3, which can be beneficial in a variety of pathologies caused by disruptions in calcium homeostasis (e.g., stroke, ischemia/reperfusion injury, and neurodegenerative diseases). Dantrolene sodium offers relief of muscle spasms, malignant hyperthermia, and antitoxic, antipyretic, and anti-inflammatory properties^{[1][2][3][4][5][6][7][8][9][10][11]}.

Dantrolene (50 μM) sodium 通过增加大鼠皮肤纤维中 ryanodine 受体 (RyR) 对 Mg²⁺ 的亲和力阻止过度活跃的 Ca²⁺ 释放，从而缓解恶性高热症^[2]。
Dantrolene (30 μM, 1 h-3 days) sodium 可改善阿尔茨海默病患者来源诱导多能干细胞的神经发生和突触生成障碍，同时恢复细胞内 ²⁺ 稳态和生理性自噬、细胞存活和增殖^[3]。
Dantrolene (40 μM, 12 h) sodium 可增强低温对大脑皮层神经元的保护作用，包括改善形态、提高存活率和线粒体膜电位、减少细胞内活性氧、细胞质组蛋白相关 DNA 断裂和细胞凋亡^[7]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Dantrolene (5-20 mg/kg, i.v.) sodium 在 Digoxin (HY-B1049) 引起的心脏毒性大鼠模型中具有心脏保护作用^[4]。
Dantrolene (5-10 mg/kg, i.p.) sodium 减轻实验性自身免疫性脑脊髓炎 (EAE) 小鼠的脊髓炎症^[5]。
Dantrolene (5 mg/kg, 鼻腔内或皮下, 每周 3 次) sodium 可以改善 5XFAD 阿尔兹海默症小鼠认知功能障碍^[6]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

336.23

C₁₄H₉N₄NaO₅

14663-23-1

固体

Yellow to orange

硝苯呋海因钠

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

• [1]. Zhang W, et al. Neuroprotective effects of dantrolene in neurodegenerative disease: Role of inhibition of pathological inflammation. J Anesth Transl Med. 2024 Jun;3(2):27-35.  [Content Brief]

  [2]. Choi RH, et al. Dantrolene requires Mg2+ to arrest malignant hyperthermia. Proc Natl Acad Sci U S A. 2017 May 2;114(18):4811-4815.  [Content Brief]

  [3]. Wang Y, et al. Dantrolene Ameliorates Impaired Neurogenesis and Synaptogenesis in Induced Pluripotent Stem Cell Lines Derived from Patients with Alzheimer's Disease. Anesthesiology. 2020 May;132(5):1062-1079.  [Content Brief]

  [4]. Zardast M, et al. Evaluation of the Effectiveness of Dantrolene Sodium against Digoxininduced Cardiotoxicity in Adult Rats. Cardiovasc Hematol Agents Med Chem. 2023;22(1):60-65.  [Content Brief]

  [5]. Osipchuk NC, et al. Modulation of Ryanodine Receptors Activity Alters the Course of Experimental Autoimmune Encephalomyelitis in Mice. Front Physiol. 2021 Dec 17;12:770820.  [Content Brief]

  [6]. Shi Y, et al. Intranasal Dantrolene as a Disease-Modifying Drug in Alzheimer 5XFAD Mice. J Alzheimers Dis. 2020;76(4):1375-1389.  [Content Brief]

  [7]. Xu SY, et al. Dantrolene enhances the protective effect of hypothermia on cerebral cortex neurons. Neural Regen Res. 2015 Aug;10(8):1279-85.  [Content Brief]

  [8]. F Zhao, et al. Dantrolene inhibition of ryanodine receptor Ca2+ release channels. Molecular mechanism and isoform selectivity. J Biol Chem. 2001 Apr 27;276(17):13810-6.  [Content Brief]

  [9]. Christopher B Sylvester, et al. Dantrolene inhibits lysophosphatidylcholine-induced valve interstitial cell calcific nodule formation via blockade of the ryanodine receptor. Front Cardiovasc Med. 2023 Mar 30:10:1112965.  [Content Brief]

  [10]. Xi Chen, et al. Dantrolene is neuroprotective in Huntington's disease transgenic mouse model. Mol Neurodegener. 2011 Nov 25;6:81.  [Content Brief]

  [11]. Büyükokuroğlu ME. Anti-inflammatory and antinociceptive properties of dantrolene sodium in rats and mice. Pharmacol Res. 2002 Jun;45(6):455-60.  [Content Brief]