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Methocarbamol is an orally bioavailable skeletal muscle relaxant.1 In vivo, methocarbamol inhibits the ability of mice to remain on a vertical ladder for 1 minute (ED50 = 15 mg/kg) and decreases forelimb grip strength by 35.9% when administered at a dose of 500 mg/kg.1,2 It abolishes femoral nerve-stimulated polysynaptic reflex contractions of the cat tibialis anterior muscle and prolongs the mean refractory period of directly or indirectly stimulated skeletal muscle when administered at a dose of 200 mg/kg.3 Methocarbamol also selectively inhibits human carbonic anhydrase (CA) isoform I over CAII (IC50s = 70 and ~80,000 μM, respectively).4 Formulations containing methocarbamol have been used to treat skeletal muscle spasms.
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1. A comparative study of the effect of some centrally acting skeletal muscle relaxants in mice. J. Pharm. Pharmacol. 26(2), 109-112 (1974).
2. Quantitative grip strength assessment as a means of evaluating muscle relaxation in mice. Psychopharmacology (Berl) 110(1-2), 92-86 (1993).
3. Some studies on peripheral actions of mephenesin, methocarbamol and diazepam. Br. J. Pharmacol. 34(3), 579-590 (1968).
4. Inhibition of carbonic anhydrases I and II by N-