|
rdf:type |
|
|
lifeskim:mentions |
|
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pubmed:issue |
6
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pubmed:dateCreated |
1981-10-29
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pubmed:abstractText |
FK-33-824 (Try-D-Ala-Gly-MePhe-Met(O)ol) is a potent enkephalin analog which has been tritium labelled with a high specific radioactivity (41 Ci/mmole). The labelled drug exhibits specific and saturable binding to rat brain crude mitochondrial fraction. Specific binding is inhibited by low concentrations of morphine, levallorphan and beta-endorphin, suggesting that FK 33-824 [3H] binds preferentially to mu opiate sites. Binding studies at equilibrium and kinetics of formation and dissociation of the labelled ligand-receptor complex indicate that FK 33-824 [3H] binds to two classes of specific sites. Their affinities are distinguishable at 0 degree (KD = 1.3 and 5.8 nM) and very close to each other at 37 degree (KD = 1.9 nM).
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|
pubmed:language |
fre
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pubmed:journal |
|
|
pubmed:citationSubset |
IM
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pubmed:chemical |
|
|
pubmed:status |
MEDLINE
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|
pubmed:month |
Jun
|
|
pubmed:issn |
0300-9084
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|
pubmed:author |
|
|
pubmed:issnType |
Print
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pubmed:volume |
63
|
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
477-84
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|
pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:6266515-Animals,
pubmed-meshheading:6266515-Brain,
pubmed-meshheading:6266515-D-Ala(2),MePhe(4),Met(0)-ol-enkephalin,
pubmed-meshheading:6266515-Endorphins,
pubmed-meshheading:6266515-Enkephalins,
pubmed-meshheading:6266515-Kinetics,
pubmed-meshheading:6266515-Levallorphan,
pubmed-meshheading:6266515-Mitochondria,
pubmed-meshheading:6266515-Morphine,
pubmed-meshheading:6266515-Papio,
pubmed-meshheading:6266515-Rats,
pubmed-meshheading:6266515-beta-Endorphin
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|
pubmed:year |
1981
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|
pubmed:articleTitle |
[Binding of a tritiated enkephalinergic analog (FK 33-824) to a mitochondrial fraction of rat brain].
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pubmed:publicationType |
Journal Article,
English Abstract,
Research Support, Non-U.S. Gov't
|
