rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
3
|
pubmed:dateCreated |
1990-4-6
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pubmed:abstractText |
Three stereoisomers of S-145 (1) with variations at the side-chain junctions were synthesized. Endo-cis isomer 10 and N-exo-trans isomer 18 were obtained via the common intermediate 5 having an endo-fused ring structure. Exo-cis isomer 28 was prepared via exo-fused azetidino compound 21. Inhibitory concentrations (IC50) of the sodium salts newly obtained for platelet aggregation were measured using washed rat platelets (WP) and human platelet-rich plasma (PRP). The IC50 values of these compounds for contraction of the rat aorta were also measured. Compound 1 of N-endo-trans structure and N-exo-trans isomer 18 exhibited more potent inhibitory activity than cis-isomers 10 and 28 against responses induced by TXA2-related substances for rat WP and rat thoracic aorta. However, these compounds exhibited almost comparable inhibitory activity for human PRP.
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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/Bicyclo Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Bridged Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Fatty Acids, Monounsaturated,
http://linkedlifedata.com/resource/pubmed/chemical/Platelet Aggregation Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Prostaglandin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Thromboxane,
http://linkedlifedata.com/resource/pubmed/chemical/S 145,
http://linkedlifedata.com/resource/pubmed/chemical/Thromboxane A2
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
|
pubmed:issn |
0022-2623
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pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:volume |
33
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1027-31
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:2137879-Animals,
pubmed-meshheading:2137879-Bicyclo Compounds,
pubmed-meshheading:2137879-Bridged Compounds,
pubmed-meshheading:2137879-Fatty Acids, Monounsaturated,
pubmed-meshheading:2137879-Humans,
pubmed-meshheading:2137879-Platelet Aggregation,
pubmed-meshheading:2137879-Platelet Aggregation Inhibitors,
pubmed-meshheading:2137879-Rats,
pubmed-meshheading:2137879-Receptors, Prostaglandin,
pubmed-meshheading:2137879-Receptors, Thromboxane,
pubmed-meshheading:2137879-Stereoisomerism,
pubmed-meshheading:2137879-Structure-Activity Relationship,
pubmed-meshheading:2137879-Thromboxane A2
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pubmed:year |
1990
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pubmed:articleTitle |
Synthesis and in vitro activity of stereoisomers of a novel thromboxane receptor antagonist, (+-)-(5Z)-7-[3-endo-[(phenylsulfonyl)amino]bicyclo [2.2.1]hept-2-exo-yl]heptenoic acid.
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pubmed:affiliation |
Shionogi Research Laboratories, Shionogi & Co., Ltd., Osaka, Japan.
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pubmed:publicationType |
Journal Article,
In Vitro
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