Differences between sodium-dependent and desipramine-defined [3H]imipramine binding in intact human platelets

Hrdina, Pavel D.

doi:10.1016/0006-3223(89)90218-7

Cited by 49 publications

(15 citation statements)

References 32 publications

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“…However, pharmacological studies in this field have shown a heterogeneity of [ 3 H]IMI binding sites when desipramine is used to define the "specific" binding (Hrdina 1989): desipramine-defined IMI binding appears to consist of two subpopulations, with only that of a proteic nature, 5-HT-sensitive and Na-dependent being present in serotonergic neurons and related to the 5-HT transporter (Marcusson et al 1985). H]PAR), a SSRI, has subsequently seemed to label the 5-HT transporter protein more specifically (Mellerup et al 1983;Marcusson et al 1988), and its use in clinical studies is currently replacing that of [ (D'Haenen et al 1988;Lawrence et al 1993;Faludi et al 1994;Maguire et al 1995;Marazziti et al 1996).…”

mentioning

confidence: 99%

Presence and Characterization of the Serotonin Transporter in Human Resting Lymphocytes

Marazziti

Rossi

Giannaccini

et al. 1998

Neuropsychopharmacology

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mentioning

confidence: 99%

Presence and Characterization of the Serotonin Transporter in Human Resting Lymphocytes

Marazziti

Rossi

Giannaccini

et al. 1998

Neuropsychopharmacology

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“…Data on the effect of age on this structure are, however, controversial. A decreased density of [ 3 H]imipramine-binding sites in elderly subjects has been reported by some authors [20,21], while others [28,29] have observed no age influence, albeit within a limited age range. While employing the [ 3 H]paroxetine binding, Andersson and Marcusson [22] did not detect any age-or sex-related effects in a group of subjects with, however, a wide range of ages.…”

Section: Discussionmentioning

confidence: 94%

Pharmacological Characterization of the Serotonin Transporter in Young and Elderly Subjects

Marazziti¹,

Baroni²,

Rossi³

et al. 2001

Neuropsychobiology

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The potency of some tricyclics (imipramine and clomipramine) and selective 5-HT reuptake inhibitors (fluoxetine, paroxetine, and citalopram) in displacing the [³H]paroxetine binding to platelet membranes was measured in young and elderly subjects of both sexes. The results showed that the most potent compound in all subjects was paroxetine, followed by clomipramine, citalopram, fluoxetine, and imipramine, with no differences between male and female subjects. All drugs, except paroxetine and clomipramine, showed significantly lower pKi values in the elderly subjects of both sexes. These findings would suggest that although the pharmacological profile of the 5-HT transporter is not modified qualitatively by age, quantitative changes in its affinity do perhaps occur which would justify more careful studies on this topic in order to get optimal dosages of drugs acting at this level.

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“…The [3H]-imipramine binding site in brain tissue has been demon strated to bind to multiple sites, where only a single high affinity (nM) site is related to the 5-HT uptake mecha nism [for review, see ref. 4], Heterogeneity of [3H]-imipramine binding has been demonstrated also for human platelets [6], Since [3H]-paroxetine can be used as a selective ligand for the 5-HT transporter in both human [8] and rat brain [7], it might also exhibit similar advan tageous characteristics in human platelets [15].…”

Section: Discussionmentioning

confidence: 99%

Inhibition and Dissociation of [<sup>3</sup>H]-Paroxetine Binding to Human Platelets

Andersson

Marcusson²

1989

Neuropsychobiology

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Previous data on dissociation studies of [³H]-imipramine and [³H]-paroxetine binding to the human platelet 5-hydroxytryptamine (5-HT, serotonin) transporter have suggested that the binding is heterogeneous in nature and/or is subject to allosteric modifications through a separate low affinity site. The platelet 5-HT transporter is often used as a biological marker in psychiatric conditions. Therefore, it was of interest to further characterize the 5-HT uptake site by using [³H]-paroxetine. The 5-HT uptake inhibitors tested (citalopram, clomipramine, imipramine, norzimeldine and paroxetine) and 5-HT itself produced competitive inhibition patterns in saturation experiments, suggesting that these agents bind to the same site. In dissociation experiments in the presence of the 5-HT uptake inhibitors, the half-time values for dissociation were the same, whereas 5-HT slowed the dissociation. These data suggest that with the concentrations used of the 5-HT uptake inhibitors, they do not modify the 5-HT transporter. However, in the presence of 5-HT, the [³H]-paroxetine dissociation is decreased, suggesting an allosteric modification of the [³H]-paroxetine binding site.

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Differences between sodium-dependent and desipramine-defined [3H]imipramine binding in intact human platelets

Cited by 49 publications

References 32 publications

Presence and Characterization of the Serotonin Transporter in Human Resting Lymphocytes

Presence and Characterization of the Serotonin Transporter in Human Resting Lymphocytes

Pharmacological Characterization of the Serotonin Transporter in Young and Elderly Subjects

Inhibition and Dissociation of [<sup>3</sup>H]-Paroxetine Binding to Human Platelets

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