Elsevier

Neuropharmacology

Volume 32, Issue 8, August 1993, Pages 737-743
Neuropharmacology

[3H]Paroxetine binding in rat frontal cortex strongly correlates with [3H]5-HT uptake: Effect of administration of various antidepressant treatments

https://doi.org/10.1016/0028-3908(93)90181-2Get rights and content

Abstract

Paroxetine is a selective and potent inhibitor of 5-hydroxytryptamine (5-HT) uptake into serotonergic neurones. [3]Paroxetine binding to rat frontal cortex was of high affinity with a high percentage of specific binding. The binding data of both competition and saturation studies fitted a single site binding model. [3H]Paroxetine binding was potently inhibited by the selective 5-HT uptake inhibitors. In addition, a very good correlation was demonstrated between the ability of twenty-three compounds to inhibit [3H]paroxetine binding to rat frontal cortical membranes and [3H]5-HT uptake into rat frontal cortical synaptosomes. These data support the view that [3H]paroxetine binds to a single site which corresponds to the 5-HT uptake site. Using this ligand, the effects of repeated administration of antidepressant drugs with a wide range of pharmacological actions and electroconvulsive shock on 5-HT reuptake sites were examined. [3H]Paroxetine binding parameters (Kd and Bmax) were unaltered by all treatments. It would, therefore, appear that antidepressant therapy does not produce adaptive changes in 5-HT uptake sites.

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