RT Journal Article
SR Electronic
T1 A COMPARISON OF THE RELATIVE TOXIC, EMETIC AND CONVULSIVE ACTIONS OF A SERIES OF METHYLATED XANTHINE DERIVATIVES
JF Journal of Pharmacology and Experimental Therapeutics
JO J Pharmacol Exp Ther
FD American Society for Pharmacology and Experimental Therapeutics
SP 343
OP 350
VO 116
IS 3
A1 J. D. McCOLL
A1 J. M. PARKER
A1 J. K. W. FERGUSON
YR 1956
UL http://jpet.aspetjournals.org/content/116/3/343.abstract
AB The acute intraperitoneal and oral toxicity in terms of LD50 mgm./kgm. was determined in the mouse for a series of 1 and 7 substituted xanthines. The values calculated for the LD50 by the intraperitoneal route in terms of mgm./kgm. varied from 100 to 1800. 1-Allyl theobromine was the most toxic derivative while 7-β-γ-dihydroxypropyl theophylline was the least toxic. By the oral route, the values for the LD50 in terms of mgm./kgm. varied from 190 to 2700. Again 1-allyl theobromine was the most toxic while 7-acetic acid theophylline was the least toxic. 7-Diethylaminoethyl theophylline was the most active derivative in producing convulsions in the mouse. Convulsions were also observed with 7-isoamyl theophylline, 7-butyl theophylline, caffeine, theophylline, aminophyffine, 1-butyl theobromine and 7-chloroethyl theophylline. By oral administration theophylline and aminophylline were well tolerated in both the dog and the cat. In both species, 1-butyl, 1-isoamyl theobromine, 7-acetic acid and 7-isoamyl theophyffine were the most active of these derivatives in producing emesis. 7-Diethylaminoethyl theophylline caused fatalities in both the dog and the cat. © 1956, by The Williams & Wilkins Company