生物活性 | |||
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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 | |||||
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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 ... 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 | |||
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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 |
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