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Journal of Pharmacology And Experimental Therapeutics, Vol. 147, Issue 3, 303-312, 1965
Copyright © 1965 by American Society for Pharmacology and Experimental Therapeutics

INTERACTION OF GUANETHIDINE WITH ADRENERGIC NEURONS

C. C. Chang 1, E. Costa 1, and B. B. Brodie 1

1 Laboratory of Chemical Pharmacology, National Heart Institute, National Institutes of Health, Bethesda, Maryland

Studies described in this paper support the view that guanethidine is localized in rat heart and spleen by unspecific binding sites and by sites specifically concerned with the storage of NE. The two types of binding may be distinguished and the specific uptake measured from the amount of guanethidine displaced by amphetamine and reserpine which selectively displace the drug from the specific sites of binding but do not affect the unspecific sites.

The specific sites are readily saturable and on increasing the dose of guanethidine these sites in heart take up a maximum of about three molecules of the drug for each molecule of contained NE.

Evidence is given for the view that the blockade of adrenergic neurons and the loss of NE from nerve endings is a consequence of the same primary action of guanethidine.

Accepted on November 2, 1964




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Copyright © 1965 by the American Society for Pharmacology and Experimental Therapeutics.