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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1-2
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pubmed:dateCreated |
1984-1-27
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pubmed:abstractText |
[3H]2-amino-4-phosphonobutyric acid was synthesized by the conjugate addition of 1-lithio-2-trimethylsilyethyne to diethyl ethynylphosphate followed by catalytic tritiation and hydrolysis. Radiolabelled 2-amino-4-phosphonobutyric acid binds to a distinct class of L-glutamate binding sites and does not exhibit appreciable binding to sites not displaced by L-glutamate. The binding affinity (Kd = 5.1 +/- 0.4 microM) and pharmacological profile correspond to those values obtained from physiological studies of 2-amino-4-phosphonobutyric acid inhibition of synaptic transmission, and to those values obtained in [3H]L-glutamate binding assays. [3H]2-amino-4-phosphonobutyric acid does not exhibit significant binding to the Cl-/Ca2+-independent L-glutamate binding site(s), nor to the Na+-dependent L-glutamate binding site (up to 50 mM Na+). These data provide further evidence that the physiological action of 2-amino-4-phosphonobutyric acid is mediated by the previously described Cl-/Ca2+-dependent L-glutamate binding sites, and provides an assay system which is optimal for the study of these sites.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/2-amino-4-phosphonobutyric acid,
http://linkedlifedata.com/resource/pubmed/chemical/Aminobutyric Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Calcium,
http://linkedlifedata.com/resource/pubmed/chemical/Chlorides,
http://linkedlifedata.com/resource/pubmed/chemical/Glutamates,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Tritium
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0006-8993
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
14
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pubmed:volume |
278
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
137-44
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:6640305-Aminobutyric Acids,
pubmed-meshheading:6640305-Animals,
pubmed-meshheading:6640305-Binding Sites,
pubmed-meshheading:6640305-Brain,
pubmed-meshheading:6640305-Calcium,
pubmed-meshheading:6640305-Cell Membrane,
pubmed-meshheading:6640305-Chlorides,
pubmed-meshheading:6640305-Glutamates,
pubmed-meshheading:6640305-Hydrogen-Ion Concentration,
pubmed-meshheading:6640305-Ligands,
pubmed-meshheading:6640305-Rats,
pubmed-meshheading:6640305-Rats, Inbred Strains,
pubmed-meshheading:6640305-Synapses,
pubmed-meshheading:6640305-Temperature,
pubmed-meshheading:6640305-Tritium
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pubmed:year |
1983
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pubmed:articleTitle |
Synthesis of [3H]2-amino-4-phosphonobutyric acid and characterization of its binding to rat brain membranes: a selective ligand for the chloride/calcium-dependent class of L-glutamate binding sites.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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