MYOTROPIC SPASMOLYTIC, HISTAMINOLYTIC, AND ATROPINELIKE ACTIONS OF SOME DERIVATIVES OF DIMETHYLAMINOETHYL BENZHYDRYL ETHER HYDROCHLORIDE (BENADRYL)

¹ From the Research Laboratories, Parke, Davis and Company, Detroit, Michigan

On the isolated quinea pig ileum and in the intact animal the acid succinate and acid oxalate of -dimethylaminoethyl benzhydryl ether have an order of histaminolytic action similar to the hydrochloride's, but the acid succinate may be less toxic (molecular comparisons). This suggestion of an anionic influence should be studied further.

Quaternary ammonium derivatives of the base, while entering the class of choline derivatives, retain potent histaminolytic properties and at the same time exhibit considerably more potent atropine-like action than salts of the tertiary type (in contrast with the known activating action of lower alkyl choline ethers). The added atropine-like action appears to increase their efficacy in protecting intact guinea pigs against death from inspired histamine mist. It is accompanied by diminished "myotropic" action and increased toxicity.

The importance of 2-carbon alkylamines in the histaminic and cholinergic as well as adrenergic systems, and the breaking down of classical boundaries of specificity in these systems concurrently with interactions between changing molecular groups are illustrated. Parallels in the relation of structure to action are drawn between the present alkamine ethers and known analogous esters.

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				T. H. McGAVACK, P. SCHULMAN, R. SCHUTZER, and H. ELIAS EFFECTS OF TOPICAL APPLICATIONS OF DIPHENHYDRAMINE HYDROCHLORIDE (BENADRYL) Arch Dermatol, March 1, 1948; 57(3_PART_I): 308 - 318. [Abstract] [PDF]