Abstract
Radioiodinated 2-hydroxy-3-(4-iodophenyl)-1-(4-phenylpiperidinyl)propane, 5 (4-HIPP), was synthesized and evaluated as a simple vesamicol-like radiotracer for mapping cholinergic pathways in the brain. Both enantiomers of 5 exhibit significant accumulation (approx. 2% of injected dose) and prolonged retention (t1/2 greater than 3 h) within the rat brain. The accumulation of radioiodinated 5 in the rat brain was reduced by up to 70% in the presence of vesamicol and its analogs. The levorotary isomer (-)-4-[123I]HIPP exhibits significant accumulation in the monkey brain, with a half-life of about 9 h. Radioiodinated 5 may therefore be a useful tool for studying cholinergic pathways in the brain.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Autoradiography
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Brain / diagnostic imaging*
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Brain / metabolism
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Cholinergic Fibers / diagnostic imaging*
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Cholinergic Fibers / metabolism
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Iodine Radioisotopes*
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Iodobenzenes / chemical synthesis*
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Iodobenzenes / metabolism
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Iodobenzenes / pharmacokinetics
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Male
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Myocardium / metabolism
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Neuromuscular Depolarizing Agents / pharmacology
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Piperidines / chemical synthesis*
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Piperidines / metabolism
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Piperidines / pharmacokinetics
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Piperidines / pharmacology
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Radionuclide Imaging
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Rats
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Rats, Inbred Strains
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Stereoisomerism
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Tissue Distribution
Substances
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Iodine Radioisotopes
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Iodobenzenes
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Neuromuscular Depolarizing Agents
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Piperidines
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2-hydroxy-3-(4-iodophenyl)-1-(4-phenylpiperidinyl)propane
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vesamicol