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Methyprylon is a sedative and hypnotic drug of the piperidinedione derivative family. It was first developed by Hoffmann-La Roche and was primarily used for the treatment of insomnia. Methyprylon acts as a positive allosteric modulator at the GABA-A receptor chloride ion channel, increasing the duration that the Cl- ionopore remains open and thereby prolonging post-synaptic inhibitory effects of GABA in the thalamus. This results in central nervous system depression with sedative-hypnotic effects similar to barbiturates but with a distinct chemical structure. The drug has largely been replaced by benzodiazepines due to their improved safety profile and fewer side effects. Methyprylon was withdrawn from major markets (US in 1975; Canada in 1990) due to adverse events including risk of overdose and toxicity[1][2][3][7].
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