Chlorzoxazone

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Chemical Structure| 95-25-0 同义名 : 氯唑沙腙 ;NSC 26189
CAS号 : 95-25-0
货号 : A300568
分子式 : C7H4ClNO2
纯度 : 99%
分子量 : 169.57
MDL号 : MFCD00005717
存储条件:

Pure form Sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Chlorzoxazone is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort. It acts on the spinal cord by depressing reflexes. Chlorzoxazone is currently being used as a marker substrate in vitro/vivo studies to quantify cytochrome P450 2E1 (CYP2E1) activity in humans[3]. Chlorzoxazone has been linked to rare instances of acute liver injury, a few of which have been fatal[4]. Chlorzoxazone (250-1000 μM) induced [Ca2+] irises in a concentration-dependent manner. Chlorzoxazone-induced Ca2+ entry was inhibited by 20% by inhibitors of store-operated Ca2+ channels and protein kinase C (PKC) modulators. In Ca2+-free medium, treatment with the endoplasmic reticulum Ca2+ pump inhibitor thapsigargin (TG) inhibited chlorzoxazone-evoked [Ca2+] irises by 88%. Chlorzoxazone at 200-700 μM decreased cell viability, which was not reversed by pretreatment with Ca2+ chelator 1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid/acetoxy methyl[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02654236 Alcohol Consumption Not Applicable Recruiting July 2019 United States, Indiana ... 展开 >> Indiana University Recruiting Indianapolis, Indiana, United States, 46202 Contact: Jennifer Lehman, RN    317-278-1872    jgeck@iu.edu    Contact: Megan Comerford, BS, MPH    3172789226    mcomerfo@iu.edu    Sub-Investigator: Naga Chalasani, MD          Principal Investigator: Suthat Liangpunsakul, MD          Sub-Investigator: David Crabb, MD 收起 <<
NCT02291666 Type 2 Diabetes Phase 4 Recruiting October 2019 Canada, Quebec ... 展开 >> Centre hospitalier de l'Université de Montréal (CHUM) Recruiting Montreal, Quebec, Canada, H2X0A9 Contact: Veronique Michaud, BPharm, PhD    514-8908000 ext 15812    v.michaud@umontreal.ca    Contact: Jacques Turgeon, BPharm,PhD    514-8908045    jacques.turgeon@umontreal.ca    Principal Investigator: Veronique Michaud, BPharm,PhD          Sub-Investigator: Jean-Louis Chiasson, MD          Sub-Investigator: Jacques Turgeon, BPharm,PhD 收起 <<
NCT00340535 - Completed - United States, Pennsylvania ... 展开 >> University of Pittsburgh Pittsburgh, Pennsylvania, United States, 15261 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.90mL

1.18mL

0.59mL

29.49mL

5.90mL

2.95mL

58.97mL

11.79mL

5.90mL

参考文献

[1]Hopf FW, Simms JA, et al. Chlorzoxazone, an SK-type potassium channel activator used in humans, reduces excessive alcohol intake in rats. Biol Psychiatry. 2011;69(7):618-24

[2]Cao Y, Dreixler JC, et al. Modulation of recombinant small-conductance Ca(2+)-activated K(+) channels by the muscle relaxant chlorzoxazone and structurally related compounds. J Pharmacol Exp Ther. 2001 Mar;296(3):683-9.

[3]Yamamura Y, Koyama N, Umehara K. Comprehensive kinetic analysis and influence of reaction components for chlorzoxazone 6-hydroxylation in human liver microsomes with CYP antibodies. Xenobiotica. 2015;45(4):353-360

[4]Chlorzoxazone. In: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; January 30, 2017

[5]Lu T, Liang WZ, Hao LJ, et al. Action of chlorzoxazone on Ca2+movement and viability in human oral cancer cells. Chin J Physiol. 2019;62(3):123-130