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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
1986-7-14
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pubmed:abstractText |
The aim of this study to was to assess the feasibility of using iodopindolol to delineate myocardial beta-adrenoreceptors in vivo. Preliminary biodistribution studies indicated that binding of 131I-d,I-pindolol in the heart was stereospecific, saturable, and displaceable by I-propranolol but not by phenoxybenzamine. However, considerable nonspecific binding was encountered. Subsequently, the stereoisomer, 131I-I-pindolol, was shown to be a high affinity beta-adrenoreceptor antagonist (Kd approximately 0.37 nM) as assessed by Scatchard analysis, and one exhibiting marked specific uptake in lung and heart in rabbits. In contrast, 131I-d-pindolol exhibited no specific binding in rabbit left ventricular membrane preparations nor specific organ uptake. Gamma camera scintigraphy with both isomers demonstrated that the I-isomer accumulated in lung and heart, and that its accumulation was blocked by I-propranolol. In contrast, d-isomer uptake was nonspecific and diffuse. The results indicate that it should be possible to externally visualize receptors by differentiating specific and nonspecific binding components of a ligand in vivo with the use of radiolabeled stereoisomers.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0161-5505
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
27
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
660-7
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:3012030-Animals,
pubmed-meshheading:3012030-Iodine Radioisotopes,
pubmed-meshheading:3012030-Male,
pubmed-meshheading:3012030-Membranes,
pubmed-meshheading:3012030-Myocardium,
pubmed-meshheading:3012030-Pindolol,
pubmed-meshheading:3012030-Rabbits,
pubmed-meshheading:3012030-Radioligand Assay,
pubmed-meshheading:3012030-Rats,
pubmed-meshheading:3012030-Rats, Inbred Strains,
pubmed-meshheading:3012030-Receptors, Adrenergic, beta,
pubmed-meshheading:3012030-Tissue Distribution
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pubmed:year |
1986
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pubmed:articleTitle |
Characterization of beta-adrenoreceptors in vivo with iodine-131 pindolol and gamma scintigraphy.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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