|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
25
|
|
pubmed:dateCreated |
1994-1-18
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|
pubmed:abstractText |
Non-peptide antagonists of the peptide hormone oxytocin (OT) with nanomolar OT receptor affinities are described. These compounds incorporate novel amido- and amidoalkylcamphor variations to the lead structure L-366,509 (1) to achieve receptor affinity enhancements of 2-3 orders of magnitude over that compound. The new OT antagonist L-367,773 (35) is shown to be an orally bioavailable agent with good duration in vivo and to inhibit OT-stimulated uterine contractions effectively in several in vitro and in vivo models.
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|
pubmed:language |
eng
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|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Dec
|
|
pubmed:issn |
0022-2623
|
|
pubmed:author |
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
10
|
|
pubmed:volume |
36
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
N
|
|
pubmed:pagination |
3993-4005
|
|
pubmed:dateRevised |
2003-11-14
|
|
pubmed:meshHeading |
pubmed-meshheading:8258821-Animals,
pubmed-meshheading:8258821-Binding Sites,
pubmed-meshheading:8258821-Female,
pubmed-meshheading:8258821-Oxytocin,
pubmed-meshheading:8258821-Piperazines,
pubmed-meshheading:8258821-Piperidines,
pubmed-meshheading:8258821-Rats,
pubmed-meshheading:8258821-Receptors, Oxytocin,
pubmed-meshheading:8258821-Spiro Compounds,
pubmed-meshheading:8258821-Structure-Activity Relationship
|
|
pubmed:year |
1993
|
|
pubmed:articleTitle |
Nanomolar-affinity, non-peptide oxytocin receptor antagonists.
|
|
pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486.
|
|
pubmed:publicationType |
Journal Article
|
