LAUSR

Baclofen, -(4-chlorophenyl)--aminobutyric acid, holds a unique position in neuroscience, remaining the only FDA approved GABAB agonist. While intended to be a more brain penetrant version of GABA (-aminobutyric acid) for the potential treatment of epilepsy, baclofen's highly efficacious muscle relaxant properties led to its approval, as a racemate, for the treatment of spasticity. Interestingly, baclofen received FDA approval before its receptor, GABAB, was discovered and its exact mechanism of action was known. In recent times, baclofen has a myriad of off-label uses, with the treatment for alcohol abuse and drug addiction garnering a great deal of attention. This article aims to capture the >60 year legacy of baclofen by walking through the history, pharmacology, synthesis, drug metabolism, routes of administration and societal impact of this Classic in chemical neuroscience.