[Characteristics of 3H-paroxetine-labeled serotonin uptake sites in rat brain].
Paroxetine (PAR) is a potent and selective inhibitor of serotonin uptake, and it has been demonstrated that 3H-PAR is a favorable candidate for labeling of the serotonin transport system. In this report, the binding of 3H-PAR to rat brain membranes was further investigated to obtain a better understanding of its role in the neuronal serotonin-uptake mechanism. Consistent with previous reports, it is indicated that 3H-PAR binds with high affinity to a site closely related to the serotonin-uptake mechanism. This binding is highly sodium dependent. The finding that depletion of brain serotonin content with p-chlorophenylalanine did not induce any alteration in the number and the affinity of the 3H-PAR-binding sites suggests the lack of serotonergic modulation on these sites. Repeated administration of desipramine, clomipramine, mianserin or deprenyl also failed to change 3H-PAR-binding sites in cerebral cortex and hippocampus. Such findings are compared to previous studies on the serotonin-uptake mechanism and the site labeled by 3H-imipramine, and discussed in respect to the biochemistry of affective disorders.
Yoshida
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Y
Department of Psychiatry and Neurology, Asahikawa Medical College, Japan.
D000818:Animals; D000928:Antidepressive Agents / Q000494:pharmacology; D001665:Binding Sites; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism*; D066298:In Vitro Techniques; D008297:Male; D017374:Paroxetine; D010880:Piperidines / Q000493:pharmacokinetics*; D051381:Rats; D011919:Rats, Inbred Strains; D012701:Serotonin / Q000493:pharmacokinetics*; D014316:Tritium
D000928:Antidepressive Agents; D010880:Piperidines; D014316:Tritium; D012701:Serotonin; D017374:Paroxetine