Abstract
THE useful autonomic ganglionic blocking agent hexamethonium, and some of its closely related derivatives, possess quaternary ammonium nitrogen atoms. The activity of the compounds of this type has commonly been associated with the quaternary ammonium salt structure. Certain side-effects of drugs of this type may also be attributed to their quaternary salt nature. In exploring a series of compounds related to W.R.L. No. 51–143, 1-methyl-3-(δ-dimethylaminobutyl)piperidine dihydrochloride, it was discovered that powerful ganglionic blocking activity is also possessed by tertiary amines. The importance of this discovery lies in the facts that not only are these tertiary amines at least as potent and much less toxic than hexamethonium derivatives, but also, lacking the quaternary salt groups of the latter compounds, they should be free of many of the aforementioned side-effects.
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NORTON, S., PHILLIPS, A. A New Type of Autonomic Blocking Agent. Nature 172, 867 (1953). https://doi.org/10.1038/172867b0
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DOI: https://doi.org/10.1038/172867b0
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