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.
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].
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