Summary
Diphenylacety Idiethylaminoethanol-hydrochloride (T), a new synthetic drug, has been assayed on barium chloride, as well as by indirect stimulation through parasympathetic nerves (acetylcholine, acetylbetamethylcholine, pilocarpine, eserine, electric stimulation of the vagus). A continuous stimulation with rise of tonus and increased contractions of the hollow viscera was provided by the slow intravenous injection of small amounts of a.c. or eserine. This method proved to be most useful for testing the relaxing effects of T as well as of other drugs. Motility of the stomach, small and large intestine, gall bladder and urinary bladder were recorded. In the case of the gall bladder relatively small doses of T produced most marked relaxation. This latter observation was confirmed in experiments on normal unanesthetized dogs reported elsewhere, in which the normal gall bladder was visualized fluoroscopically and in which T relaxed the resting as well as the physiologically contracted gall bladder (5). A comparison of the M.L.D. and of effective relaxing doses of atropine and of T reveals that a relatively smaller dose of T is more effective in causing relaxation. T in doses found to be non-toxic in normal animals compared well with the effects of 1 mg. of atropine sulfate and 2.5 mg. of papaverine hydrochloride administered in a number of experiments (see Table I and III, and Fig. 2). The effect of T (10–20 mg.) on salivary secretion of the dog was found to be slight and transient, while 1 mg. of atropine sulfate abolished it completely. In trials on ourselves 150 mg. of T per os produced no perceptible dryness of the mouth.
Thus, in principle, our experiments support the re varlcus animals. Its toxicity has been determined on the rat and the dog.
In the anesthetized dog doses above 12 mg. depress blood-pressure. T abolishes the vasodepressor effect of acetylcholine just as does atropine in the noneserinized and eserinized animal.
T abolishes or diminishes gastric hunger contractions in normal unanesthetized dogs.
T diminishes or abolishes spasm and contraction of stomach, small and large intestine produced by various drugs or vagus stimulation in anesthetized dogs.
In the case of the gall bladder contracted by various drugs or electric stimulation of the vagi, T has a striking relaxing effect in comparitively small doses.
T counteracts the contracting effects of pilocarpine on the urinary bladder.
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Necheles, H., Neuwelt, F., Steiner, N. et al. Study of a new spasmolytic drug: diphenylacetyldiethylaminoethanolhydrochloride (Trasentili). American Journal of Digestive Diseases 6, 39–46 (1939). https://doi.org/10.1007/BF02996620
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DOI: https://doi.org/10.1007/BF02996620