Evidence is provided to indicate that the distribution coefficients of various barbituric acids can be related to the number of carbon atoms and the Taft polar constants of the 5,5-substituents. This suggests that the hydrophilic portion of the molecule is affected not only by the size of the substituents but, also, by their polarity.
Halothane was labeled with tritium (Wilzbach method) by exposure to 2.3 curies of tritium gas for fourteen days. The one hydrogen of the molecule was labeled and on purification gave a final specific activity of 2.9 mc. per Gm. In the preparation a considerable amount of ‘loose’ tritium and highly active impurities were separated and the purity of the final product following gas chromatographic purification was better than 99.95 per cent.
In the course of an investigation into the applicability of a quantitative potassium bromide disk method to various drugs and chemicals, the cinchona alkaloids, quinidine, quinine, cinchonine, and cinchonidine were studied. Under certain experimental conditions, possibly due to the formation of dimorphous and amorphous forms, anomalous spectra were obtained for quinidine and quinine. Cinchonine and cinchonidine did not exhibit significant variations in spectra under the conditions investigated.
The unnatural nucleoside, psicofuranine, is bimolecularly hydrolyzed by acid to adenine and the sugar psicose. Adenine appears to reverse the biological activity of psicofuranine in the plate-disk method against S. aureus so that standard curves must be prepared with the same amount of adenine as the material to be assayed. When this phenomenon is accounted for, the chemical and biological assays are shown to correlate. The kinetic constants for the acid catalyzed hydrolysis of the nucleoside have been determined.
The plan of this investigation was to complex tetracaine HCl and some related local anesthetics with certain metal ions; and to determine the most acceptable complexing metal ions, the stability constants of the metal complexes under varying conditions, and the biological significance of such complexes.
Of seven psychopharmacologic drugs screened by five assay procedures, only meprobamate ana phenaglycodol exhibited significant anticonvulsant activity. Chlorpromazine, promazine, reserpine, and hydroxyzine lowered the threshold for minimal seizures variously induced, whereas triflupromazine had no effect on seizure threshold. The data obtained correlate well with available clinical data and indicate the value of threshold seizure studies in animals for detecting agents which may cause convulsions in man.
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