Abstract
The cocaine analogue RTI-121 (3 beta-(4-iodophenyl)tropane-2 beta-carboxylic acid isopropyl ester), when labeled with carbon-11, was evaluated in rats as a potential PET ligand for the dopamine transporter. The compound gave in vivo striatum:cerebellum ratios that were similar to those obtained with the related ligand [11C]RTI-55 (2 beta-(4-iodophenyl)tropane-2 beta-carboxylic acid methyl ester) but showed a much greater selectivity for the dopamine compared with the 5-HT uptake site. The results indicate that [11C]RTI-121 could be used in preference to [11C]RTI-55 in man. Experimentally, [11C]RTI-121 has potential in the quantification of dopamine terminal function in rat models of disease, using a combination of autoradiography, postmortem sampling, and in vivo tomography.
MeSH terms
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Animals
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Biotransformation
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Blood Proteins / metabolism
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Brain / diagnostic imaging*
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Brain / metabolism*
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Carbon Radioisotopes*
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Carrier Proteins / analysis
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Carrier Proteins / metabolism*
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Cerebellum / metabolism
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Cocaine / analogs & derivatives*
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Cocaine / metabolism
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Cocaine / pharmacokinetics
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Corpus Striatum / metabolism
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Dopamine / metabolism
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Dopamine Plasma Membrane Transport Proteins
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Male
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Membrane Glycoproteins*
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Membrane Transport Proteins*
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Nerve Tissue Proteins*
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Radioligand Assay
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Rats
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Rats, Sprague-Dawley
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Tissue Distribution
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Tomography, Emission-Computed / methods*
Substances
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Blood Proteins
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Carbon Radioisotopes
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Carrier Proteins
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Dopamine Plasma Membrane Transport Proteins
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Membrane Glycoproteins
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Membrane Transport Proteins
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Nerve Tissue Proteins
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RTI 121
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Cocaine
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Dopamine