β Scribed by Harald G. O. Holck; Marvin H. Malone; Hideko Katayama Kaji
No coin nor oath required. For personal study only.
The n-propyl-(PBB), ethyl-(EBB), and methyl-(MBB) homologs of propallylonal (IPBB) were prepared. Using albino rats, the intraperitoneal ED5,,s and LD,os were determined, as well as PDSos 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-methylbuty1)barbituric acid. Interand 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.
lyl) barbituric acid is an unusual hypnotic in that injection of hypnotic doses usually causes a high incidence of delayed deaths in rats one to five days later. Such deaths may even follow subhypnotic doses (1,2). This death is commonly accompanied by pronounced edema of the lungs with labored respiration, by hepatizatilm, and by pneumonia. Fatty infiltration of the liver, kidneys, heart, and lungs, ataxia, anorexia, and emaciation may also occur. Delayed deaths following propallylonal did not occur in the earliest experiments done with the rat according to Vogt (3); however, Boedecker and Ludwig (4) reported occasional delayed deaths in the rabbit after large oral doses of a homolog, butallylonal. Fitch and Tatum (1) described delayed effects in the rat leading to death in a few days, and Holck and co-workers carried out a series of investigations dealing with the consistent occurrence of delayed death in a variety of albino and hybrid rat stocks in Beirut, Chicago, and
π SIMILAR VOLUMES
were comparatively smaller presumably due to further oxidative degradation of the five-membered heterocyclic ring carrying the epoxy group. Ecgonine and Cocaine-Ecgonine is a carboxy derivative of tropanol, while cocaine is a carbomethoxy derivative of tropanyl benzoate. Although these compounds wo