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  • Pharmacologic Study of Alkyl 2-Bromoallyl Barbituric Acids
  • Add time:07/21/2019         Source:sciencedirect.com

    The n-propyl-(PBB), ethyl-(EBB), and methyl-(MBB) homologs of propallylonal (IPBB) were prepared. Using albino rats, the intraperitoneal ED50s and LD50s were determined, as well as PD50s against pentylenetetrazol. Effectiveness in developing tolerance and cross-tolerance against propallylonal by feeding low concentrations in the diet for two weeks was in decreasing order: EBB, probarbital, IPBB, PBB, MBB, and 5-(2-bromoallyl)-5-(1-methylbutyl)barbituric acid. Inter- and intralaboratory variations occurred as to incidence of delayed death (EBB, IPBB) and in sex variation (IPBB). Rat electrocardiograms taken after administration of the bromoallyl barbiturates revealed no significant changes. In mice, PBB was most effective and IPBB least effective in protecting against a surely fatal dose of strychnine when given at various intervals of time after the barbiturate. None of the bromoallyl barbiturates gave complete protection when given one hour before a dosage range of 2.5–20.2 mg./Kg. of strychnine sulfate subcutaneously. Phenobarbital sodium was superior to the bromoallyl compounds against strychnine lethality.

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