Abstract
The present study compares the anorectic activity of d-fenfluramine and its metabolite d-norfenfluramine in three animal species. d-Fenfluramine and d-norfenfluramine show anorectic activity at increasing doses (ED50) in rats, guinea pigs, and mice, d-norfenfluramine being more active than d-fenfluramine in all three species. Equiactive anorectic activities are reached with different brain levels of d-fenfluramine and d-norfenfluramine, guinea pigs being the most sensitive species, followed by rats then mice. The metabolite most probably plays a major role in the anorectic effect of d-fenfluramine in guinea pigs, contributes to the anorectic activity in rats, but adds little to the action of the parent drug in mice. The different sensitivity to d-fenfluramine and d-norfenfluramine in these three species does not appear to be explained by a number of biochemical parameters, including serotonin uptake or release, receptor subtypes, or 3H-d-fenfluramine binding and uptake.
Original language | English |
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Pages (from-to) | 483-490 |
Number of pages | 8 |
Journal | Naunyn-Schmiedeberg's Archives of Pharmacology |
Volume | 343 |
Issue number | 5 |
DOIs | |
Publication status | Published - May 1991 |
Keywords
- Anorectics
- d-Fenfluramine
- Guinea pigs
- Mice
- Rats
- Serotonin
- Serotonin receptors
- Serotonin release
- Serotonin uptake
ASJC Scopus subject areas
- Pharmacology