| 货号 | 18869-25g |
| 描述 | Chlorzoxazone is a benzoxazolone derivative that causes skeletal muscle relaxation and blocks spasticity in clinical studies.1,2 Chlorzoxazone enhances small and intermediate conductance calcium-activated potassium channels (EC50s = 87 and 98 µM for KCa2.2 and KCa3.1, respectively).3,4 The cytochrome P450 isoform CYP2E1 converts chlorzoxazone to 6-hydroxy chlorzoxazone (Item No. 10009029). The urinary excretion of this 6-hydroxy metabolite is often used as a probe of CYP2E1 activity in studies of hepatotoxicity.5,6,7 |
| 别名 | NSC 26189; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Chou, R.,Peterson, K. and Helfand, M. Comparative efficacy and safety of skeletal muscle relaxants for spasticity and musculoskeletal conditions: A systematic review. Journal of Pain and Symptom Management 28(2), 140-175 (2004). 2.See, S. and Ginzburg, R. Choosing a skeletal muscle relaxant. American Family Physician 78(3), 365-370 (2008). 3.Pedarzani, P. and Stocker, M. Molecular and cellular basis of small- and intermediate-conductance, calcium-activated potassium channel function in the brain. Cellular and Molecular Life Sciences 65(20), 3196-3217 (2008). 4.Gao, Z.,Todorov, B.,Barrett, C.F., et al. Cerebellar ataxia by enhanced Cav2.1 currents is alleviated by Ca+2-dependent K+-channel activators in CacnalaS218L mutant mice. Journal of Neuroscience 32(44), 15533-15546 (2012). 5.Court, M.H.,Von Moltke, L.L.,Shader, R.I., et al. Biotransformation of chlorzoxazone by heptic microsomes from humans and ten other mammalian species. Biopharmaceutics & Drug Disposition 18, 213-226 (1997). 6.Frye, R.F.,Adedoyin, A.,Mauro, K., et al. Use of chlorzoxazone as an in vivo probe of cytochrome P450 2E1: Choice of dose and phenotypic trait measure. Journal of Clinical Pharmacology 38, 82-89 (1998). 7.Peter, R.,Bocker, R.,Beaune, P.H., et al. Hydroxylation of chlorzoxazone as a specific probe for human liver cytochrome P450 2E1. Chemical Research in Toxicology 3, 566-573 (1990). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 169.6 |
| 分子式 | C7H4ClNO2 |
| CAS号 | 95-25-0 |
| 稳定性 | ≥ 2 years |
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