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Journal of Pharmacology And Experimental Therapeutics, Vol. 165, Issue 1, 9-13, 1969
Copyright © 1969 by American Society for Pharmacology and Experimental Therapeutics

METABOLISM OF SOME PHENYLETHYLAMINES AND THEIR beta-HYDROXYLATED ANALOGS IN BRAIN

GEORGE R. BREESE 1, THOMAS N. CHASE 1, and IRWIN J. KOPIN 1

1 Laboratory of Clinical Science, National Institute of Mental Health, Bethesda, Maryland

In rat brain slices, phenylethylamine derivatives were converted predominantly to acidic metabolites, whereas the beta-hydroxylated derivatives (norepinephrine, normetanephrine and octopamine) were converted predominantly to neutral metabolites. Normetanephrine-H3 incubated with guinea-pig brain slices was converted mainly to 3-methoxy-4-hydroxyphenylglycol, whereas normetanephrine incubated with liver slices was metabolized primarily to 3-methoxy-4-hydroxymandelic acid. Studies comparing metabolism of i.v. and intracisternally injected normetanephrine indicate that reduction of the intermediate aldehyde is the predominant route of metabolism of beta-hydroxylated phenylethylamine derivatives in vivo as well as in vitro in brain tissue.

Submitted on June 7, 1968
Accepted on September 16, 1968




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