rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
1985-10-17
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pubmed:abstractText |
The synthesis and binding properties to rat brain tissue of the enkephalinase inhibitor [3H] N-[(R,S)-3-hydroxyaminocarbonyl-2-benzyl-1-oxopropyl]-glycine ([3H]HACBO-Gly, 45 Ci/mmole) is reported. [3H]HACBO-Gly binding to membranes from various rat brain tissue is saturable (KD = 0.4 +/- 0.05 nM) and linearly related to the amount of tissue. Non specific binding is less than 15% of total binding at the KD concentration. The regional distribution of [3H]HACBO-Gly binding and enkephalinase activity are closely correlated with highest levels in striatum and substantia nigra. The efficiency of inhibitors of various peptidases (thiorphan, captopril, bestatin ...) to inhibit [3H]HACBO-Gly binding or enkephalinase activity are similar. These results indicate that [3H]HACBO-Gly binds selectively to enkephalinase. This compound should help to clarify the localization of the enzyme in the CNS.
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pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
|
pubmed:issn |
0006-291X
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pubmed:author |
|
pubmed:issnType |
Print
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pubmed:day |
30
|
pubmed:volume |
131
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
262-8
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:3899113-Animals,
pubmed-meshheading:3899113-Brain,
pubmed-meshheading:3899113-Captopril,
pubmed-meshheading:3899113-Cell Membrane,
pubmed-meshheading:3899113-Corpus Striatum,
pubmed-meshheading:3899113-Glycine,
pubmed-meshheading:3899113-Hydroxylamines,
pubmed-meshheading:3899113-Leucine,
pubmed-meshheading:3899113-Male,
pubmed-meshheading:3899113-Neprilysin,
pubmed-meshheading:3899113-Protease Inhibitors,
pubmed-meshheading:3899113-Rats,
pubmed-meshheading:3899113-Rats, Inbred Strains,
pubmed-meshheading:3899113-Substantia Nigra,
pubmed-meshheading:3899113-Thiorphan,
pubmed-meshheading:3899113-Tiopronin,
pubmed-meshheading:3899113-Tissue Distribution
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pubmed:year |
1985
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pubmed:articleTitle |
Binding of the bidentate inhibitor [3H]HACBO-Gly to the rat brain neutral endopeptidase "enkephalinase".
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
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