Central effects of N-allyl,N'-methyl-barbital and N-allylmethyprylon in mice

Pharmacological activities (hypnotic, anticonvulsant and convulsant activities, acute toxicity and pentobarbital (PB) synergism) of N-allyl,N'-methyl derivatives of barbiturates and related N-allyl substituted compounds were studied in mice. N-Allylhexobarbital (AHB), N-allylglutethimide (AGI) and N-allylmethyprylon (AMP) showed hypnotic activity. N-Allyl,N'-methyl derivatives of barbital (B), phenobarbital (PheB) and PB (AMB, AMPheB and AMPB), AHB and AMP exhibited anticonvulsant activity against pentylenetetrazol (PTZ)-induced seizures. AMP was the most potent agent among the allyl compounds tested in the protective effect against PTZ-induced seizures. N-Allyl, N'-methylallobarbital (AMAlloB) showed a weak convulsant activity at a dose of 640 mg/kg, i.p. All allyl compounds tested showed potentiation of the PB-induced sleep. AMB prolonged the PB-induced sleep 30-fold as compared with the control. These results indicate that AMB, AMP and the other N-allyl compounds possess some depressant effects on the central nervous system.