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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
13
|
pubmed:dateCreated |
1995-8-17
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pubmed:abstractText |
The design and synthesis of a new class of potent and selective 5-HT4 receptor agonists containing an indole nucleus linked to a carbazimidamide are presented. A conformational study of the 5-HT4 receptor agonists serotonin and zacopride led to the identification of an initial pharmacophore and to the definition of a three-dimensional map of the 5-HT4 agonist recognition site. 1, a representative member of our new class of 5-HT4 receptor agonists, incorporates all reference structural features and matched perfectly with these models. 1 is a highly potent, full agonist at 5-HT4 receptors present in the isolated electrically stimulated guinea pig ileum preparation, with a pD2 value of 8.8, displaying selectivity (ranging from 40- to over 10,000-fold) versus other members of the serotonin receptor family.
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pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Jun
|
pubmed:issn |
0022-2623
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
23
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pubmed:volume |
38
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
2326-30
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:7608898-Animals,
pubmed-meshheading:7608898-Binding Sites,
pubmed-meshheading:7608898-Drug Design,
pubmed-meshheading:7608898-Guinea Pigs,
pubmed-meshheading:7608898-Ileum,
pubmed-meshheading:7608898-Molecular Conformation,
pubmed-meshheading:7608898-Receptors, Serotonin,
pubmed-meshheading:7608898-Serotonin Receptor Agonists
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pubmed:year |
1995
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pubmed:articleTitle |
The serotonin 5-HT4 receptor. 1. Design of a new class of agonists and receptor map of the agonist recognition site.
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pubmed:affiliation |
Sandoz Pharma Limited, Basel, Switzerland.
|
pubmed:publicationType |
Journal Article,
In Vitro
|