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Journal of Pharmacology And Experimental Therapeutics, Vol. 86, Issue 1, 7-13, 1946
Copyright © 1946 by American Society for Pharmacology and Experimental Therapeutics

THE ANTI-HISTAMINE ACTION OF ALKYLOXYTRIAZINES AND RELATED COMPOUNDS

EARL R. LOEW 1, MARGARET E. KAISER 1, and MONA ANDERSON 1

1 From the Division of Pharmacological Research, Parke, Davis and Company Research Laboratories, Detroit 32, Michigan

Among a series of twenty-four 2-substituted diaminotriazines, several (propoxy, isopropoxy, isobutoxy, sec.-butoxy and cyclohexoxy) were found to be four times as efficacious as aminophylline in preventing experimental asthma induced in guinea pigs with atomized histamine. These triazine ethers are less potent than phenolic ethers and benzhydryl ethers with respect to anti-histamine action as tested on bronchiolar smooth muscle. The ratio of LD-50 in mice to minimal effective dose in guinea pigs was 25 to 40 for alkyloxydiaminotriazines, as compared with only 5 for aminophylline.

Alkyloxytriazines prevented spasm of guinea pig intestinal muscle which ordinarily follows addition of histamine, barium, or acetylcholine to the muscle bath. The anti-histamine action of three triazines tested on intestinal tissue was two to ten times that of aminophylline. These compounds are not specific histamine antagonists for the spasmogenic effects of barium and acetylcholine were also antagonized by dilutions of drug comparable to those effective against histamine.

Submitted on August 8, 1945






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Copyright © 1946 by the American Society for Pharmacology and Experimental Therapeutics.