Abstract
[18F]-N-(p-nitrobenzyl)spiperone, [18F]PNBS, was prepared and its in vivo uptake in rat brain was measured. A temporal increase in striatum:cerebellum ratio and frontal cortex:cerebellum (FC:Cb) ratio was observed. Blocking studies suggested the formation of a radiolabeled metabolite, presumably [18F]spiperone, that is capable of crossing the blood-brain barrier and labeling cortical 5-HT2 receptors. This was confirmed using the ISRP method of metabolite analysis indicating [18F]PNBS is not a suitable tracer for studying D2 receptors in vivo with PET.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Brain / metabolism
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Chromatography, High Pressure Liquid
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Fluorine Radioisotopes*
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Isotope Labeling
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Ligands
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Nitrobenzenes / chemical synthesis*
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Nitrobenzenes / metabolism
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Rats
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Rats, Sprague-Dawley
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Receptors, Dopamine D2 / metabolism
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Spiperone / analogs & derivatives*
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Spiperone / chemical synthesis
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Spiperone / metabolism
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Tissue Distribution
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Tomography, Emission-Computed
Substances
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Fluorine Radioisotopes
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Ligands
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Nitrobenzenes
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Receptors, Dopamine D2
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N-(4-nitrobenzyl)spiperone
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Spiperone
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3-N-methylspiperone