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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
8
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pubmed:dateCreated |
1993-11-9
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pubmed:abstractText |
Paroxetine is a selective and potent inhibitor of 5-hydroxytryptamine (5-HT) uptake into serotonergic neurones. [3H]Paroxetine binding to rat frontal cortex was of high affinity with a high percentage of specific binding. The binding data of both competition and saturation studies fitted a single site binding model. [3H]Paroxetine binding was potently inhibited by the selective 5-HT uptake inhibitors. In addition, a very good correlation was demonstrated between the ability of twenty-three compounds to inhibit [3H]paroxetine binding to rat frontal cortical membranes and [3H]5-HT uptake into rat frontal cortical synaptosomes. These data support the view that [3H]paroxetine binds to a single site which corresponds to the 5-HT uptake site. Using this ligand, the effects of repeated administration of antidepressant drugs with a wide range of pharmacological actions and electroconvulsive shock on 5-HT reuptake sites were examined. [3H]Paroxetine binding parameters (Kd and Bmax) were unaltered by all treatments. It would, therefore, appear that antidepressant therapy does not produce adaptive changes in 5-HT uptake sites.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Aug
|
pubmed:issn |
0028-3908
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pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
32
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pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
737-43
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:8413837-Animals,
pubmed-meshheading:8413837-Antidepressive Agents,
pubmed-meshheading:8413837-Binding, Competitive,
pubmed-meshheading:8413837-Electroshock,
pubmed-meshheading:8413837-Kinetics,
pubmed-meshheading:8413837-Male,
pubmed-meshheading:8413837-Membranes,
pubmed-meshheading:8413837-Paroxetine,
pubmed-meshheading:8413837-Prefrontal Cortex,
pubmed-meshheading:8413837-Rats,
pubmed-meshheading:8413837-Rats, Sprague-Dawley,
pubmed-meshheading:8413837-Serotonin,
pubmed-meshheading:8413837-Serotonin Uptake Inhibitors,
pubmed-meshheading:8413837-Synaptosomes
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pubmed:year |
1993
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pubmed:articleTitle |
[3H]paroxetine binding in rat frontal cortex strongly correlates with [3H]5-HT uptake: effect of administration of various antidepressant treatments.
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pubmed:affiliation |
Boots Pharmaceuticals Research Department, Nottingham, U.K.
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pubmed:publicationType |
Journal Article,
In Vitro
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