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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2001-6-15
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pubmed:abstractText |
The pharmacological effect of a novel selective 5-HT4 receptor agonist, TS-951 (N-[endo-8-(3-hydroxypropyl)-8-azabicyclo[3.2.1]oct-3-yl]-1-isopropyl-2-oxo-1,2-dihydro-3-quinolinecarboxamide) was investigated in vitro. TS-951 potently inhibited specific [3H]GR113808 binding both in guinea-pig striatum and in mouse brain. The affinity of TS-951 for the 5-HT4 receptor was higher than those of other agonists, 5-HT, cisapride, mosapride and renzapride. On the longitudinal muscle of the guinea-pig ileum, TS-951 caused a concentration-dependent increase in the amplitude of electrically induced submaximal twitch contractions. On the longitudinal muscle of the guinea-pig distal colon, TS-951 also caused concentration-dependent contractions. TS-951 is a high-affinity, selective and potent 5-HT4 receptor agonist. This compound therefore can be considered as a useful pharmacological tool for investigating 5-HT4 receptor-mediated events.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/GR 113808,
http://linkedlifedata.com/resource/pubmed/chemical/Indoles,
http://linkedlifedata.com/resource/pubmed/chemical/Quinolines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Neurotransmitter,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin, 5-HT4,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Receptor Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Sulfonamides,
http://linkedlifedata.com/resource/pubmed/chemical/TS951
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0031-7012
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pubmed:author |
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pubmed:copyrightInfo |
Copyright 2001 S. Karger AG, Basel
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pubmed:issnType |
Print
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pubmed:volume |
63
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
8-16
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:11408827-Animals,
pubmed-meshheading:11408827-Brain,
pubmed-meshheading:11408827-Colon,
pubmed-meshheading:11408827-Corpus Striatum,
pubmed-meshheading:11408827-Guinea Pigs,
pubmed-meshheading:11408827-Ileum,
pubmed-meshheading:11408827-Indoles,
pubmed-meshheading:11408827-Male,
pubmed-meshheading:11408827-Mice,
pubmed-meshheading:11408827-Mice, Inbred ICR,
pubmed-meshheading:11408827-Molecular Structure,
pubmed-meshheading:11408827-Muscle, Smooth,
pubmed-meshheading:11408827-Muscle Contraction,
pubmed-meshheading:11408827-Quinolines,
pubmed-meshheading:11408827-Radioligand Assay,
pubmed-meshheading:11408827-Receptors, Neurotransmitter,
pubmed-meshheading:11408827-Receptors, Serotonin,
pubmed-meshheading:11408827-Receptors, Serotonin, 5-HT4,
pubmed-meshheading:11408827-Serotonin Antagonists,
pubmed-meshheading:11408827-Serotonin Receptor Agonists,
pubmed-meshheading:11408827-Sulfonamides
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pubmed:year |
2001
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pubmed:articleTitle |
Pharmacological characterization of a novel 5-HT4 receptor agonist, TS-951, in vitro.
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pubmed:affiliation |
Pharmacology Lab., Pharmaceut. Res. Lab., Taisho Pharmaceut. Co. Ltd, Ohmiya, Saitama, Japan.
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pubmed:publicationType |
Journal Article,
In Vitro
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