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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
9
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pubmed:dateCreated |
1984-10-3
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pubmed:abstractText |
A series of substituted 4-aryltetrahydrothieno[2,3-c]pyridines was prepared by acid-catalyzed cyclization of 1-aryl-2-[(2-thienylmethyl)amino]ethanol derivatives. The compounds were examined for their antidepressant activity, as demonstrated by their ability to inhibit the uptake of norepinephrine (NE) and serotonin (5-HT) and to prevent tetrabenazine-induced ptosis (TBZ) in mice. Significant inhibition of both neurotransmitters is observed for several of the tested compounds, while some of them are selective inhibitors of either NE or 5-HT uptake. Optimal activity is associated with the introduction of lipophilic substituents into the 4-position of the phenyl ring and less lipophilic substituents into the 2-position of the thiophene ring (11, 23). Compound 33 bearing substituents in positions 2 and 6 of the phenyl ring is inactive. This might be a consequence of an out of plane conformation of this compound.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antidepressive Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Nomifensine,
http://linkedlifedata.com/resource/pubmed/chemical/Norepinephrine,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridines,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Thiophenes
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
27
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1150-5
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:6471069-Animals,
pubmed-meshheading:6471069-Antidepressive Agents,
pubmed-meshheading:6471069-Biological Transport,
pubmed-meshheading:6471069-Models, Molecular,
pubmed-meshheading:6471069-Nomifensine,
pubmed-meshheading:6471069-Norepinephrine,
pubmed-meshheading:6471069-Pyridines,
pubmed-meshheading:6471069-Rats,
pubmed-meshheading:6471069-Serotonin,
pubmed-meshheading:6471069-Structure-Activity Relationship,
pubmed-meshheading:6471069-Thiophenes
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pubmed:year |
1984
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pubmed:articleTitle |
Synthesis and antidepressant activity of 4-aryltetrahydrothieno[2,3-c]pyridine derivatives.
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pubmed:publicationType |
Journal Article
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