Chronic administration of different antidepressant drugs reduced the number of [3H]imipramine [( 3H]IMI) binding sites in rat cerebral cortex. In the same experimental conditions, fluvoxamine and dothiepin, as well as desmethylimipramine, induced an increase in the maximal velocity of high affinity serotonin (5HT) uptake in cortical slices, whereas citalopram and viloxazine were ineffective in this regard. Our results indicate that even if 5HT uptake and [3H]IMI binding sites are located on the same nerve terminals, they are differently modulated. Increased Vmax of the 5HT uptake process could be due to a rebound phenomenon after withdrawal from drugs that acutely inhibit 5HT uptake. The effect on [3H]IMI sites might be explained through either the agonist properties of the drugs towards these sites or the involvement of mechanisms still unknown.

Effect of some tricyclic and nontricyclic antidepressants on [3H]imipramine binding and serotonin uptake in rat cerebral cortex after prolonged treatment / N. Brunello, M. Riva, A. Volterra, G. Racagni. - In: FUNDAMENTAL & CLINICAL PHARMACOLOGY. - ISSN 0767-3981. - 1:5(1987), pp. 327-333.

Effect of some tricyclic and nontricyclic antidepressants on [3H]imipramine binding and serotonin uptake in rat cerebral cortex after prolonged treatment

M. Riva
Secondo
;
G. Racagni
Ultimo
1987

Abstract

Chronic administration of different antidepressant drugs reduced the number of [3H]imipramine [( 3H]IMI) binding sites in rat cerebral cortex. In the same experimental conditions, fluvoxamine and dothiepin, as well as desmethylimipramine, induced an increase in the maximal velocity of high affinity serotonin (5HT) uptake in cortical slices, whereas citalopram and viloxazine were ineffective in this regard. Our results indicate that even if 5HT uptake and [3H]IMI binding sites are located on the same nerve terminals, they are differently modulated. Increased Vmax of the 5HT uptake process could be due to a rebound phenomenon after withdrawal from drugs that acutely inhibit 5HT uptake. The effect on [3H]IMI sites might be explained through either the agonist properties of the drugs towards these sites or the involvement of mechanisms still unknown.
Rats, Inbred Strains; Rats; Cerebral Cortex; Animals; Imipramine; Protein Binding; Serotonin; Nerve Tissue Proteins; Male; Antidepressive Agents; Antidepressive Agents, Tricyclic
Settore BIO/14 - Farmacologia
1987
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/183574
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