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rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0001041,
umls-concept:C0030685,
umls-concept:C0205464,
umls-concept:C0231491,
umls-concept:C0391871,
umls-concept:C0680255,
umls-concept:C1143376,
umls-concept:C1176028,
umls-concept:C1176472,
umls-concept:C1283071,
umls-concept:C1880022,
umls-concept:C1963578
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|
pubmed:issue |
7
|
|
pubmed:dateCreated |
2003-3-20
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|
pubmed:abstractText |
A small series of aryl pyridyl sulfones has been prepared and investigated for its 5-HT(6) receptor binding properties. Thereof, pyrrolidinyl derivative 11 proved to be a very potent (pK(i) 9) and selective 5-HT(6) receptor antagonist. By means of in vivo microdialysis in the frontal cortex and a passive avoidance paradigm, where 11 reversed a scopolamine induced retention deficit, a functional correlation between 5-HT(6) receptors and cholinergic neurotransmission could be shown, supporting the therapeutic potential of 5-HT(6) receptors in the treatment of cognitive deficits.
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pubmed:language |
eng
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pubmed:journal |
|
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pubmed:citationSubset |
IM
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pubmed:chemical |
|
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pubmed:status |
MEDLINE
|
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pubmed:month |
Mar
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pubmed:issn |
0022-2623
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pubmed:author |
|
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pubmed:issnType |
Print
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pubmed:day |
27
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pubmed:volume |
46
|
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pubmed:owner |
NLM
|
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1273-6
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:12646038-Acetylcholine,
pubmed-meshheading:12646038-Administration, Oral,
pubmed-meshheading:12646038-Animals,
pubmed-meshheading:12646038-Avoidance Learning,
pubmed-meshheading:12646038-Biological Availability,
pubmed-meshheading:12646038-Blood-Brain Barrier,
pubmed-meshheading:12646038-Cell Line,
pubmed-meshheading:12646038-Frontal Lobe,
pubmed-meshheading:12646038-Half-Life,
pubmed-meshheading:12646038-Humans,
pubmed-meshheading:12646038-Injections, Intravenous,
pubmed-meshheading:12646038-Microdialysis,
pubmed-meshheading:12646038-Microsomes, Liver,
pubmed-meshheading:12646038-Pyridines,
pubmed-meshheading:12646038-Rats,
pubmed-meshheading:12646038-Receptors, Serotonin,
pubmed-meshheading:12646038-Serotonin Antagonists,
pubmed-meshheading:12646038-Sulfones,
pubmed-meshheading:12646038-Tissue Distribution
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pubmed:year |
2003
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pubmed:articleTitle |
Influence of the 5-HT6 receptor on acetylcholine release in the cortex: pharmacological characterization of 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine, a potent and selective 5-HT6 receptor antagonist.
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pubmed:affiliation |
F. Hoffmann-LaRoche, Pharma Division, Preclinical Research, CH-4070 Basel, Switzerland.
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pubmed:publicationType |
Journal Article,
In Vitro
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