THE EFFECTS OF XYLAMINE, A NITROGEN-MUSTARD ON [H-3]NOREPINEPHRINE ACCUMULATION IN RABBIT AORTA

  • 1 January 1980
    • journal article
    • research article
    • Vol. 214  (2) , 324-327
Abstract
Xylamine (N-2-chloroethyl-N-ethyl-2-methylbenzylamine) irreversibly inhibits [3H]norepinephrine accumulation by rabbit aortic rings in vitro. Inhibition is observed when aortic rings are exposed to xylamine, washed and [3H]norepinephrine accumulation is measured in media free of xylamine. This dose-dependent effect, with an I50 [median inhibitory concentration] of 10-7 M, is prevented by coincubation of xylamine with the reversible uptake inhibitors cocaine and amphetamine in the incubation bath during exposure of the tissue to xylamine. The action of xylamine is Na-dependent, as when tissue was exposed to xylamine in Na-free Krebs'' solution, xylamine had no action. Reduction of K ion concentration and the presence of ouabain protected against xylamine inhibition. Xylamine action involves interaction with the neuronal uptake system in a manner very similar to norepinephrine.