| Inhibition and dissociation of [3H]-paroxetine binding to human platelets. | |
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MedLine Citation:
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PMID: 2535005 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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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Authors:
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A Andersson; J Marcusson |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Neuropsychobiology Volume: 22 ISSN: 0302-282X ISO Abbreviation: Neuropsychobiology Publication Date: 1989 |
Date Detail:
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Created Date: 1990-12-04 Completed Date: 1990-12-04 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 7512895 Medline TA: Neuropsychobiology Country: SWITZERLAND |
Other Details:
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Languages: eng Pagination: 135-40 Citation Subset: IM |
Affiliation:
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Department of Geriatric Medicine, University of Umeå Sweden. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Antidepressive Agents* Binding, Competitive / physiology Blood Platelets / metabolism* Dose-Response Relationship, Drug Humans Paroxetine Piperidines / pharmacokinetics* Receptors, Serotonin / metabolism* Serotonin / blood Serotonin Antagonists* |
| Chemical | |
Reg. No./Substance:
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0/Antidepressive Agents; 0/Piperidines; 0/Receptors, Serotonin; 0/Serotonin Antagonists; 50-67-9/Serotonin; 61869-08-7/Paroxetine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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