|5-氯苯并[d]恶唑-2(3H)-酮|CsnPharm

CAS No.: 95-25-0

Chlorzoxazone/氯唑沙宗 Catalog No. CSN13101

Synonyms: NSC 26189;Paraflex;5-Chloro-2-benzoxazolone

Chlorzoxazone, a potassium channel activator, is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort. It is also a CYP2E1 inhibitor with IC50 value of 1.03μM.

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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 ... more >> 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 Collapse <<
NCT02291666	Type 2 Diabetes	Phase 4	Recruiting	October 2019	Canada, Quebec ... more >> 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 Collapse <<
NCT00340535	-	-	Completed	-	United States, Pennsylvania ... more >> University of Pittsburgh Pittsburgh, Pennsylvania, United States, 15261 Collapse <<

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 5.8973 mL
- 29.4863 mL
- 58.9727 mL
- 5 mM
- 1.1795 mL
- 5.8973 mL
- 11.7945 mL
- 10 mM
- 0.5897 mL
- 2.9486 mL
- 5.8973 mL

技术信息

CAS号

95-25-0

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C7H4ClNO2

运输

蓝冰

分子量

169.57

别名

NSC 26189;Paraflex;5-Chloro-2-benzoxazolone;Chlorzoxazon;Myoflexin;Parafon;Forte;DSC;氯唑沙宗

溶解度

DMSO	32.0 mg/mL (188.7 mM)
Water	Insoluble
Ethanol	33.0 mg/mL (194.6 mM)

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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 ... more >> 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 Collapse <<
NCT02291666	Type 2 Diabetes	Phase 4	Recruiting	October 2019	Canada, Quebec ... more >> 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 Collapse <<
NCT00340535	-	-	Completed	-	United States, Pennsylvania ... more >> University of Pittsburgh Pittsburgh, Pennsylvania, United States, 15261 Collapse <<
NCT03103568	Drug Drug Interaction	Phase 1	Completed	-	Germany ... more >> PAREXEL EPCU Berlin Berlin, Germany, 14050 Collapse <<
NCT00330434	Alcohol Drinking ... more >> Depression Smoking Cessation Attention Deficit Disorder Collapse <<	Not Applicable	Completed	-	United States, Massachusetts ... more >> Tufts University School of Medicine Boston, Massachusetts, United States, 02111 Collapse <<
NCT01187862	Cytochrome Ph... more >>armacokinetics Collapse <<	Phase 1	Completed	-	Switzerland ... more >> University Hospital Basel, Switzerland, 4031 Collapse <<
NCT00138684	Insulin Resistance ... more >> Iron Overload Collapse <<	Phase 2	Completed	-	France ... more >> CHU Nantes Nantes, France Unité d'Investigation Clinique - Hôpital Pontchaillou Rennes, France, 35033 Collapse <<
NCT03563287	Obesity, Morbid ... more >> Bariatric Surgery Candidate Collapse <<	Not Applicable	Completed	-	Finland ... more >> University of Eastern Finland Kuopio, Finland Collapse <<
NCT02405104	Osteoarthritis of Hip ... more >> Osteoarthritis, Knee Collapse <<	Phase 4	Active, not recruiting	May 2019	Denmark ... more >> Northern Orthopaedic Division, Clinik Farsoe, Aalborg University Hospital Farsoe, Northern Jutland, Denmark Collapse <<
NCT01342341	-	-	Completed	-	-
NCT01933542	Chlorzoxazone ... more >> Postoperative Pain Collapse <<	Phase 4	Completed	-	Denmark ... more >> Glostrup University Hospital Glostrup, Denmark, 2600 Collapse <<
NCT01342341	Alcohol Abuse	Phase 4	Completed	-	United States, California ... more >> Ernest Gallo Clinic and Research Center Emeryville, California, United States, 94608 Collapse <<

Chlorzoxazone/氯唑沙宗 Catalog No. CSN13101

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