Imipramine inhibits the serotonin uptake by binding with high affinity to regulatory sites of this uptake located on axons that release serotonin. The number of imipramine recognition sites located on crude synaptic membrane preparations is reduced by two daily injections of imipramine or desmethylimipramine for 3 weeks. When the binding sites for [3H]imipramine are down-regulated the Vmax of the neuronal uptake of serotonin is increased. Moreover, in minces prepared from the brain hippocampus of rats receiving imipramine in a dose regimen that reduces the number of [3H]imipramine recognition sites, the efficiency of imipramine as a blocker of the serotonin uptake is diminished. Hence the high-affinity binding sites for [3H]imipramine may have a physiological role in modulation of serotonin reuptake. Probably this is mediated by an endogenous effector of these regulatory sites. A nonpeptidic constituent of rat brain capable of displacing [3H]imipramine from its high-affinity binding site and of inhibiting the serotonin uptake in a dose-related manner has been extracted and its partial purification is described.

Barbaccia, M.l., Gandolfi, O., Chuang, D., Costa, E. (1983). Modulation of neuronal serotonin uptake by a putative endogenous ligand of imipramine recognition sites. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 80(16), 5134-5138.

Modulation of neuronal serotonin uptake by a putative endogenous ligand of imipramine recognition sites

BARBACCIA, MARIA LUISA;
1983-08-01

Abstract

Imipramine inhibits the serotonin uptake by binding with high affinity to regulatory sites of this uptake located on axons that release serotonin. The number of imipramine recognition sites located on crude synaptic membrane preparations is reduced by two daily injections of imipramine or desmethylimipramine for 3 weeks. When the binding sites for [3H]imipramine are down-regulated the Vmax of the neuronal uptake of serotonin is increased. Moreover, in minces prepared from the brain hippocampus of rats receiving imipramine in a dose regimen that reduces the number of [3H]imipramine recognition sites, the efficiency of imipramine as a blocker of the serotonin uptake is diminished. Hence the high-affinity binding sites for [3H]imipramine may have a physiological role in modulation of serotonin reuptake. Probably this is mediated by an endogenous effector of these regulatory sites. A nonpeptidic constituent of rat brain capable of displacing [3H]imipramine from its high-affinity binding site and of inhibiting the serotonin uptake in a dose-related manner has been extracted and its partial purification is described.
Pubblicato
Rilevanza internazionale
Articolo
Sì, ma tipo non specificato
Settore BIO/14
English
Con Impact Factor ISI
Axons; Fluoxetine; Hippocampus; Male; Synaptic Membranes; Imipramine; Rats; Animals; Carrier Proteins; Serotonin; Kinetics; Receptors, Neurotransmitter; Biological Transport; Neurons; Receptors, Drug; Rats, Inbred Strains
Barbaccia, M.l., Gandolfi, O., Chuang, D., Costa, E. (1983). Modulation of neuronal serotonin uptake by a putative endogenous ligand of imipramine recognition sites. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 80(16), 5134-5138.
Barbaccia, Ml; Gandolfi, O; Chuang, D; Costa, E
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2108/15005
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