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DOPAMINE‐β‐OXIDASE ACTIVITY IN MAN, USING HYDROXYAMPHETAMINE AS SUBSTRATE
Author(s) -
SJOERDSMA A.,
STUDNITZ W.
Publication year - 1963
Publication title -
british journal of pharmacology and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0366-0826
DOI - 10.1111/j.1476-5381.1963.tb01467.x
Subject(s) - metabolite , chemistry , hydroxylation , pharmacology , in vivo , active metabolite , endocrinology , urine , dopamine , medicine , enzyme , biochemistry , biology , microbiology and biotechnology
Hydroxy amphetamine was administered orally to five human subjects in daily doses of 26 to 118 mg. Approximately half the dosage administered was recoverable in the urine as unchanged drug (free plus conjugated) and 3.7 to 9.1% was excreted as the β‐hydroxylated metabolite, hydroxynorephedrine (free plus conjugated). Since conversion of hydroxyamphetamine to hydroxynorephedrine occurs in vitro by the action of dopamine‐β‐oxidase, a simple method is suggested for measuring the activity of this enzyme and the effect of its inhibitors in man. No impairment of β‐hydroxylation was noted in an adrenalectomized subject. The β‐hydroxylation of hydroxyamphetamine in vivo has not been described previously.