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  • 1
    ISSN: 1435-1463
    Keywords: 3H-imipramine ; 3H-paroxetine ; human brain ; suicide victims
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The binding of 3H-paroxetine and 3H-imipramine has been compared in 17 different regions of 12 human control brains. Our findings reveal that the regional distribution is similar for both radioligands and their bindings tend to be parallel in the brain. The highest binding site density was found in basal ganglia (hypothalamus Bmax 780 ± 102 fmol/mg protein for 3H-imipramine binding and Bmax 515∼ 83 for 3H-paroxetine binding). The lowest values were found in cortical areas (cingulate cortex 191 ± 18.5 fmol/mg for 3H-imipramine binding and 88 ± 7.5 fmol/mg for 3H-paroxetine binding). The Kd values for 3H-paroxetine binding to neuronal membranes were similar in all brain regions (mean ± s.d. Kd 0.07 ± 0.007 nM) and also for 3H-imipramine binding (mean ± s.d. Kd 1.05 ± 0.12 nM). As these values are the same as in platelet membrane, the results obtained indicate that both binding sites are identical in neuronal and in platelet membranes. These findings suggest that both ligands are good markers of the 5HT transporter. However, the higher affinity of 3H-paroxetine confirms that this compound is a better radioligand for the 5HT uptake site.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1435-1463
    Keywords: [3H]imipramine ; [3H]paroxetine ; human brain ; depression ; suicide
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Specific binding of [3H]imipramine and [3H]paroxetine was simultaneously examined in human brains (frontal cortex, temporal cortex, cingulate cortex, hypothalamus, hippocampus and amygdala) from 11 controls and 11 depressed suicide victims. A single saturable high affinity site was obtained for both radioligands. Age was not related to significant changes in [3H]imipramine and [3H]paroxetine binding parameters, which indicates the stability of the brain serotonergic system with increasing age. A major finding of the present study concerns the existence of a significant decrease in the maximum number (Bmax) of [3H]imipramine binding sites in hippocampus from depressed suicides as compared with the control group, without changes in the binding affinity (Kd). In contrast, when [3H]paroxetine was used as radioligand, no changes in either Bmax or Kd were detected in any of the brain regions studied. These findings suggest that [3H]imipramine may be a better marker than [3H]paroxetine when alterations in the presynaptic serotonergic uptake site are to be detected.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
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