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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
1989-4-6
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pubmed:abstractText |
Atrial natriuretic peptides (ANPs) are degraded rapidly by renal brush border membranes in vitro. Here, we report that thiorphan, a specific inhibitor of endopeptidase 24.11, afforded almost complete protection against inactivation of ANPs by a renal brush border membrane preparation. The diastereoisomers of [3-(N-hydroxy)carboxamido-2-benzylpropanoyl]-L-alanine (HCBA) are potent inhibitors of endopeptidase 24.11 and were also tested for their abilities to inhibit ANP-(103-126) degradation. The (S,S)-diastereoisomer was more effective than the (R,S)-diastereoisomer (kelatorphan), but both were less potent than thiorphan. To determine if endopeptidase inhibitors could decrease ANP metabolism in in vivo, thiorphan and (S,S)-HCBA were given to rats with or without a continuous infusion of ANP-(103-126). Both inhibitors induced rapid increases in plasma ANP concentration in rats administered exogenous ANP-(103-126), but had no effect on endogenous ANP levels. Thus, specific inhibitors of endopeptidase 24.11 decrease the degradation of ANPs in vitro, and are effective in reducing the metabolism of ANP-(103-126) in vivo.
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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/Atrial Natriuretic Factor,
http://linkedlifedata.com/resource/pubmed/chemical/Dipeptides,
http://linkedlifedata.com/resource/pubmed/chemical/Neprilysin,
http://linkedlifedata.com/resource/pubmed/chemical/Protease Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Thiorphan,
http://linkedlifedata.com/resource/pubmed/chemical/kelatorphan
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0303-7207
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
61
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
201-8
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:2521834-Animals,
pubmed-meshheading:2521834-Atrial Natriuretic Factor,
pubmed-meshheading:2521834-Dipeptides,
pubmed-meshheading:2521834-Kidney,
pubmed-meshheading:2521834-Male,
pubmed-meshheading:2521834-Microvilli,
pubmed-meshheading:2521834-Neprilysin,
pubmed-meshheading:2521834-Protease Inhibitors,
pubmed-meshheading:2521834-Rabbits,
pubmed-meshheading:2521834-Rats,
pubmed-meshheading:2521834-Thiorphan
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pubmed:year |
1989
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pubmed:articleTitle |
Specific inhibitors of endopeptidase 24.11 inhibit the metabolism of atrial natriuretic peptides in vitro and in vivo.
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pubmed:affiliation |
Searle Research and Development, G.D. Searle & Co., Chesterfield, MO 63198.
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pubmed:publicationType |
Journal Article
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