Abstract
Abstract The antihypertensive and myocardial noradrenaline-depleting activities of the three identified guanethidine metabolites were compared with those of guanethidine itself. Metabolite A (guanethidine-N-oxide) and Metabolite B [2-(6-carboxylamino)ethylguanidine] both showed approximately 1/30th of the antihypertensive effect of guanethidine in rats. Metabolite A, but not Metabolite B, caused a depletion of cardiac noradrenaline stores. The intensity of this effect was between 1/10th and 1/30th that of guanethidine. Metabolite C [(6-carboxyhexyl)-2-iminoimidazolidine] was inactive on both parameters. [3H]Noradrenaline uptake into isolated bovine nerve granules was not impaired by either guanethidine or its metabolites. It is concluded that the antihypertensive and myocardial noradrenaline depleting effects of guanethidine are produced by the unchanged drug rather than by one of the identified metabolites.
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