Chlorzoxazone

Mechanism of action:
Chlorzoxazone is a centrally acting muscle relaxant. Chlorzoxazone mainly acts at the level of the spinal cord and brainstem within the central nervous system. It influences small conductance calcium-activated potassium channels (SK channels), promoting potassium efflux and causing hyperpolarization of neuronal membrane potential. This reduces the excitability of spinal motor neurons, particularly by suppressing the activity of polysynaptic reflex arcs, thereby producing muscle relaxation and reducing spasticity.
Reference(s):
1. Dong DL et al. (2006). Chlorzoxazone inhibits contraction of rat thoracic aorta. Eur J Pharmacol.
2. Park JY et al. (2006). Effect of high-dose aspirin on CYP2E1 activity in healthy subjects measured using chlorzoxazone as a probe. J Clin Pharmacol.
3. Wan J et al. (2006). Chlorzoxazone metabolism is increased in fasted Sprague-Dawley rats. J Pharm Pharmacol.
