Abstract
D-Fenfluramine, fluoxetine and sertraline are considered to be serotoninergic appetite-suppressive drugs. These three agents have been compared in fasted mice, rats and guinea pigs for their activity as food intake inhibitors. D-Fenfluramine is the most effective drug in the three animal species followed by fluoxetine and then sertraline. All three compounds are metabolized to N-dealkylated metabolites which accumulate in the brain and are themselves effective in reducing food intake. At anorectic doses the brain levels of the drugs and their metabolites are compatible with the concentrations able to block serotonin (5-HT) uptake and to release brain 5-HT from brain synaptosomes. However only the anorectic activity of D-fenfluramine is antagonized by the previous administration of 5-HT antagonists. These results cast some doubts on the role of brain 5-HT in explaining the anorectic activity of fluoxetine and sertraline.
| Original language | English |
|---|---|
| Journal | International Journal of Obesity |
| Volume | 16 |
| Issue number | SUPPL. 4 |
| Publication status | Published - 1992 |
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Keywords
- Anorexia
- D-fenfluramine
- Fluoxetine
- Food intake
- Serotonin receptors
- Serotonin uptake
- Serotoninergic drugs
- Sertraline
ASJC Scopus subject areas
- Food Science
- Endocrinology
- Medicine (miscellaneous)
- Endocrinology, Diabetes and Metabolism
- Public Health, Environmental and Occupational Health
Cite this
An update on the pharmacology of serotoninergic appetite-suppressive drugs. / Garattini, S.
In: International Journal of Obesity, Vol. 16, No. SUPPL. 4, 1992.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - An update on the pharmacology of serotoninergic appetite-suppressive drugs
AU - Garattini, S.
PY - 1992
Y1 - 1992
N2 - D-Fenfluramine, fluoxetine and sertraline are considered to be serotoninergic appetite-suppressive drugs. These three agents have been compared in fasted mice, rats and guinea pigs for their activity as food intake inhibitors. D-Fenfluramine is the most effective drug in the three animal species followed by fluoxetine and then sertraline. All three compounds are metabolized to N-dealkylated metabolites which accumulate in the brain and are themselves effective in reducing food intake. At anorectic doses the brain levels of the drugs and their metabolites are compatible with the concentrations able to block serotonin (5-HT) uptake and to release brain 5-HT from brain synaptosomes. However only the anorectic activity of D-fenfluramine is antagonized by the previous administration of 5-HT antagonists. These results cast some doubts on the role of brain 5-HT in explaining the anorectic activity of fluoxetine and sertraline.
AB - D-Fenfluramine, fluoxetine and sertraline are considered to be serotoninergic appetite-suppressive drugs. These three agents have been compared in fasted mice, rats and guinea pigs for their activity as food intake inhibitors. D-Fenfluramine is the most effective drug in the three animal species followed by fluoxetine and then sertraline. All three compounds are metabolized to N-dealkylated metabolites which accumulate in the brain and are themselves effective in reducing food intake. At anorectic doses the brain levels of the drugs and their metabolites are compatible with the concentrations able to block serotonin (5-HT) uptake and to release brain 5-HT from brain synaptosomes. However only the anorectic activity of D-fenfluramine is antagonized by the previous administration of 5-HT antagonists. These results cast some doubts on the role of brain 5-HT in explaining the anorectic activity of fluoxetine and sertraline.
KW - Anorexia
KW - D-fenfluramine
KW - Fluoxetine
KW - Food intake
KW - Serotonin receptors
KW - Serotonin uptake
KW - Serotoninergic drugs
KW - Sertraline
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UR - http://www.scopus.com/inward/citedby.url?scp=0027076012&partnerID=8YFLogxK
M3 - Article
VL - 16
JO - International Journal of Obesity
JF - International Journal of Obesity
SN - 0307-0565
IS - SUPPL. 4
ER -