Dec 1, 1957

The ethyleneiminium ion as the active species in 2-haloalkylamine compounds

British Journal of Pharmacology and Chemotherapy
J D GRAHAM

Abstract

Certain 2-haloethylamine compounds which exert antagonism to adrenaline and noradrenaline of the type shown by dibenamine have been examined. The compounds were N-ethyl-N-chlorobenzyl-2-chloroethylamine hydrochlorides in which the Cl is in the p-, o-, and m- positions of the benzene ring, and the three related ethyleneiminium picrylsulphonates. In addition the Cl- and Br- compounds of the N-ethyl-N-9-fluorenyl-2-haloethylamine hydrohalide series were examined. For the haloethylamines, a curve was provided which showed the relation between probable production and decay of ethyleneiminium ion in neutralized solution with time. A correlation was established between the shape of this curve and the curve relating anti-adrenaline and anti-noradrenaline activity of samples of solutions of these compounds treated in an identical way. The relation to antagonism of histamine and 5-hydroxytryptamine was not so exact and varied with species.The ethyleneiminium ions of the three chlorobenzyl compounds exerted a typical long-lasting non-competitive antagonism to the pressor actions of adrenaline and noradrenaline. They also antagonized the effect of 5-hydroxytryptamine and histamine on blood pressure. The ED50 of the ion when administered as...Continue Reading

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Mentioned in this Paper

Histamine Measurement
Exertion
Amines
Serotonin
Epinephrine Measurement
Norepinephrine
Norepinephrine Measurement
Haloalkylamine
Blood Pressure
Allergy Testing Histamine (Lab Test)

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