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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
1983-11-23
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pubmed:abstractText |
A novel high affinity radioiodinated photoaffinity probe, 4-amino-6,7-dimethoxy-2[4-[5(3-[125I]iodo-4-azidophenyl)pentanoyl]-1- piperazinyl]-quinazoline, structurally related to the potent alpha 1-adrenergic antagonist prazosin, was developed and used to covalently label the rat cerebral cortex alpha 1-adrenergic receptor. In the absence of light, this ligand binds to cortex plasma membranes with a dissociation constant of 308 pM and with a maximal number of binding sites of 200 fmol/mg protein. Upon photolysis, the ligand incorporates irreversibly into plasma membrane proteins. Autoradiograms of such membrane samples subjected to sodium dodecyl sulfate-polyacrylamide gel electrophoresis reveal a major specifically labeled polypeptide at Mr = 79,000. The covalent incorporation into the peptide at Mr = 79,000 can be inhibited by several adrenergic receptor ligands with a typical alpha 1-adrenergic receptor specificity and stereoselectivity.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Sep
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pubmed:issn |
0006-291X
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
30
|
pubmed:volume |
115
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pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
946-51
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:6313003-Affinity Labels,
pubmed-meshheading:6313003-Animals,
pubmed-meshheading:6313003-Azides,
pubmed-meshheading:6313003-Cell Membrane,
pubmed-meshheading:6313003-Cerebral Cortex,
pubmed-meshheading:6313003-Kinetics,
pubmed-meshheading:6313003-Male,
pubmed-meshheading:6313003-Rats,
pubmed-meshheading:6313003-Rats, Inbred Strains,
pubmed-meshheading:6313003-Receptors, Adrenergic, alpha
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pubmed:year |
1983
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pubmed:articleTitle |
Covalent labeling of the cerebral cortex alpha 1-adrenergic receptor with a new high affinity radioiodinated photoaffinity probe.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
|