|
rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0079284,
umls-concept:C0205177,
umls-concept:C0205250,
umls-concept:C0205531,
umls-concept:C0226896,
umls-concept:C0231491,
umls-concept:C0243076,
umls-concept:C0442027,
umls-concept:C0762126,
umls-concept:C1414262,
umls-concept:C1527415,
umls-concept:C1720127,
umls-concept:C1880355,
umls-concept:C2348358
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|
pubmed:issue |
13
|
|
pubmed:dateCreated |
1999-1-29
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|
pubmed:abstractText |
The discovery, in vitro and in vivo studies of the highly potent ETA antagonist EMD 122946 are presented. This compound displayed high binding affinity and functional antagonism [IC50 = 3.2 x 10(-11) M, pA2 = 9.5 (ETA)] and inhibited the ET-1 induced pressor response in pithed rats with an ED50 of 0.3 mg/kg. In conscious spontaneously hypertensive rats and in DOCA-salt hypertensive rats the compound lowered mean blood pressure with an ED50 of 0.06 mg/kg. EMD 122946 exhibited high bioavailability in rats and monkeys.
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|
pubmed:language |
eng
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|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Jul
|
|
pubmed:issn |
0960-894X
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|
pubmed:author |
|
|
pubmed:issnType |
Print
|
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pubmed:day |
7
|
|
pubmed:volume |
8
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
1771-6
|
|
pubmed:dateRevised |
2004-1-20
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|
pubmed:meshHeading |
pubmed-meshheading:9873432-Animals,
pubmed-meshheading:9873432-Biological Availability,
pubmed-meshheading:9873432-Blood Pressure,
pubmed-meshheading:9873432-Endothelin-1,
pubmed-meshheading:9873432-Rats,
pubmed-meshheading:9873432-Receptor, Endothelin A,
pubmed-meshheading:9873432-Receptors, Endothelin,
pubmed-meshheading:9873432-Swine,
pubmed-meshheading:9873432-Thiazoles
|
|
pubmed:year |
1998
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|
pubmed:articleTitle |
Endothelin antagonists: discovery of EMD 122946, a highly potent and orally active ETA selective antagonist.
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|
pubmed:affiliation |
Merck KGaA, Preclinical Pharmaceutical Research, Grafing, Germany. mederski@merck.de
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pubmed:publicationType |
Journal Article
|
