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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
6
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pubmed:dateCreated |
1993-12-23
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pubmed:abstractText |
[125I]RTI-55 is a newly synthesized cocaine congener that may offer advantages over other ligands previously used to examine cocaine binding sites. However, the in vitro pharmacological and anatomical characterization of [125I]RTI-55 binding sites has not been previously performed in human brain. To determine the specificity, stability, and feasibility of [125I]RTI-55 for use in radioligand binding assays in postmortem human tissue, a series of experiments were performed characterizing [125I]RTI-55 binding sites in human brain using homogenized membrane preparations and quantitative autoradiography. Analysis of the association, dissociation, and saturation data favored two-phase processes. A curve-fitting analysis of the data derived in saturation experiments found a high-affinity site with KD = 66 +/- 35 pM and Bmax = 13.2 +/- 10.1 pmol/g of tissue and a low-affinity site with KD = 1.52 +/- 0.55 nM and Bmax of 47.5 +/- 11.2 pmol/g of tissue. Competition by ligands known to bind to the dopamine transporter showed a rank order of RTI-55 > GBR-12909 > maxindol > WIN 35428 > = methylphenidate > (-)-cocaine > buproprion > (+)-amphetamine. Binding to serotonergic sites was evaluated in the midbrain. Results of the saturation experiment performed autoradiographically in the midbrain showed a single site with KD = 370 +/- 84 pM. It appears that [125I]RTI-55 should be useful in further studies of the regulation of cocaine binding sites using postmortem human specimens.
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pubmed:grant |
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Carrier Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Cocaine,
http://linkedlifedata.com/resource/pubmed/chemical/Dopamine Plasma Membrane Transport...,
http://linkedlifedata.com/resource/pubmed/chemical/Iodine Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Membrane Glycoproteins,
http://linkedlifedata.com/resource/pubmed/chemical/Membrane Transport Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Nerve Tissue Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/RTI 55,
http://linkedlifedata.com/resource/pubmed/chemical/SLC6A4 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Plasma Membrane...
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0022-3042
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
61
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1996-2006
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:8245956-Adult,
pubmed-meshheading:8245956-Autoradiography,
pubmed-meshheading:8245956-Binding, Competitive,
pubmed-meshheading:8245956-Binding Sites,
pubmed-meshheading:8245956-Carrier Proteins,
pubmed-meshheading:8245956-Caudate Nucleus,
pubmed-meshheading:8245956-Cell Membrane,
pubmed-meshheading:8245956-Cocaine,
pubmed-meshheading:8245956-Corpus Striatum,
pubmed-meshheading:8245956-Dopamine,
pubmed-meshheading:8245956-Dopamine Plasma Membrane Transport Proteins,
pubmed-meshheading:8245956-Female,
pubmed-meshheading:8245956-Humans,
pubmed-meshheading:8245956-Iodine Radioisotopes,
pubmed-meshheading:8245956-Kinetics,
pubmed-meshheading:8245956-Male,
pubmed-meshheading:8245956-Membrane Glycoproteins,
pubmed-meshheading:8245956-Membrane Transport Proteins,
pubmed-meshheading:8245956-Middle Aged,
pubmed-meshheading:8245956-Nerve Tissue Proteins,
pubmed-meshheading:8245956-Serotonin,
pubmed-meshheading:8245956-Serotonin Plasma Membrane Transport Proteins
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pubmed:year |
1993
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pubmed:articleTitle |
[125I]RTI-55 binding to cocaine-sensitive dopaminergic and serotonergic uptake sites in the human brain.
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pubmed:affiliation |
Department of Psychiatry, University of North Carolina at Chapel Hill.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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