<i>N</i>-ethyl-α-methyl-α-(m-trifluoromethylbenzyl)nitron—the major <i>in vitro</i> metabolic product of fenfluramine in guinea-pig liver microsomal fractions

Beckett, A. H.; Coutts, Ronald T.; Ogunbona, F. A.

doi:10.1111/j.2042-7158.1973.tb10622.x

Cited by 23 publications

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“…Schuster et al(l986) stated that fenfluramine "is not changed into an active metabolite" in guinea-pigs and concluded after showing that fenfluramine caused long-term depletion of brain 5-HT in guinea-pigs that metabolism to norfenfluramine is not required in order for fenfluramine to produce long-term depletion of brain 5-HT. Their belief that fenfluramine was not metabolized to norfenfluramine in guinea-pigs was based on a paper by Beckett et al(1973), who reported that the nitrone was the major metabolite when fenfluramine was incubated with guinea-pig liver microsomes in-vitro but did not study fenfluramine metabolism in-vivo. No data on whether fenfluramine is metabolized to norfenfluramine in guinea-pigs in-vivo appear to have been published.…”

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Metabolism of fenfluramine to norfenfluramine in guinea-pigs

Fuller

Snoddy

Perry

1988

Journal of Pharmacy and Pharmacology

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After injection of fenfluramine into guinea-pigs, the N-dealkylated metabolite norfenfluramine was present in brain at higher concentrations and persisted longer than the parent drug, fenfluramine. Contrary to a claim in previous literature, the guinea-pig does metabolize fenfluramine to norfenfluramine, hence the ability of fenfluramine to cause acute and long-term depletion of brain 5-hydroxytryptamine in this species does not prove that fenfluramine, instead of nonfenfluramine, can produce these effects.

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confidence: 99%