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Methocarbamol is a central muscle relaxant used to treat skeletal muscle spasms. Under the trade name Robaxin, it is marketed by Actient Pharmaceuticals in the United States and Pfizer in Canada. Methocarbamol produces its clinical effects through agonism of the GABAA receptor, resulting in an exaggerated effect of gamma-aminobutyric acid (GABA) which occurs naturally in the brain. Activation of the GABA receptor increases the amount of chloride ions that pass through the chloride channel of cells, resulting in a depressant effect by reducing the cells action potential (like dimming a light, the cell continues to function but at a lower capacity). This mechanism is very similar to that of barbiturates, benzodiazepines, z-drugs, alcohol, and GABA analogues such as GHB. Most GABAergics require GABA as a co-factor in order to activate the chloride channel, however methocarbamol can activate the chloride channel even in the absence of GABA; this ability is called direct agonism (as opposed to allosteric agonism) and is relatively rare among GABAergic drugs, being shared only by other carbamate derivatives and a handful of other substances.
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