Document Detail

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

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