Edward R. Atkinson

Chapter 32. Antiradiation Agents

Publisher Summary This chapter describes the advances in the development of antiradiation agents. The methods used for the evaluation of antiradiation drugs have been summarized. The complexities that arise in the use of whole animals as test systems are as prevalent as in other areas of pharmacology. A series of 144 N-substituted S-2-aminoethyl thiosulfates was prepared. Many members gave good protection to mice at doses of 0.07–0.1 Of the LD 50 . A comparison of the pharmacology of a series of Bunte salts with that of the related aminothiols showed that the Bunte salts were less toxic to mice but that the differences in radioprotective potency between members of each series could not be predicted accurately. The optimum spacing between the amino and thiosulfate groups was two carbon atoms. The dose-reduction factor was not increased by the concurrent administration of serotonin. S-[2-(3-ethylaminopropylamino)ethyl]-dihydrogenphosphorothioate and the related 3-methylamino compound protected mice as effectively as the related compound having no substituent on the terminal nitrogen atom. The dose-reduction factor for dimethylsulfoxide (DMSO) absorbed through the tails of mice was found to be 1.35.