Repeated treatment with d-fenfluramine or metergoline alters cortex binding of 3H-serotonin and serotenergic sensitivity in rats.
28-day treatment with d-fenfluramine, a serotonin (5HT) releaser and uptake inhibitor, caused significant reduction (23%) of 3H-5HT binding sites (Bmax) in the rat cortex. These sites were significantly increased (31%) in cortical membranes of rats which had received metergoline, a potent serotonin antagonist, for 28 days. Parallel changes were found in the anorectic activity of metachlorophenylpiperazine (m-CPP), a potent central 5HT agonist: chronic treatment with d-fenfluramine or metergoline caused respectively a decrease and in the effect of m-CPP on food intake. The data show that changes in 5HT central receptor number and sensitivity may occur after chronic treatment with drugs acting on brain serotonin.
D000818:Animals; D001067:Appetite Depressants; D001665:Binding Sites / Q000187:drug effects; D002540:Cerebral Cortex / Q000378:metabolism*; D004873:Ergolines / Q000494:pharmacology*; D005260:Female; D005277:Fenfluramine / Q000494:pharmacology*; D008711:Metergoline / Q000494:pharmacology*; D010879:Piperazines / Q000494:pharmacology; D051381:Rats; D011985:Receptors, Serotonin / Q000187:drug effects*; D012701:Serotonin / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000494:pharmacology; D013997:Time Factors
D001067:Appetite Depressants; D004873:Ergolines; D010879:Piperazines; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D008711:Metergoline; D005277:Fenfluramine; D012701:Serotonin; C015068:1-(3-chlorophenyl)piperazine