title: Synthesis and in vivo evaluation of [18F]-N-(p-nitrobenzyl)spiperone ([18F]PNBS) in rats.
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.
authors: Cerebrovascular Research Center, University of Pennsylvania, Philadelphia 19104.
authors: R H
authors: RH
authors: Mach
authors: P A
authors: PA
authors: Nowak
authors: D A
authors: DA
authors: Moroney
authors: T E
authors: TE
authors: Morton
authors: J R
authors: JR
authors: Jackson
authors: R L
authors: RL
authors: Ehrenkaufer
mesh_terms: D000818:Animals; D001921:Brain / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D005462:Fluorine Radioisotopes; D007553:Isotope Labeling; D008024:Ligands; D009578:Nitrobenzenes / Q000138:chemical synthesis* / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D017448:Receptors, Dopamine D2 / Q000378:metabolism; D013134:Spiperone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000378:metabolism; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed
chemical_list: D005462:Fluorine Radioisotopes; D008024:Ligands; D009578:Nitrobenzenes; D017448:Receptors, Dopamine D2; C081030:N-(4-nitrobenzyl)spiperone; D013134:Spiperone; C039167:3-N-methylspiperone