Synthesis and in vivo evaluation of [18F]-N-(p-nitrobenzyl)spiperone ([18F]PNBS) in rats.
[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.
Mach
R H
RH
Cerebrovascular Research Center, University of Pennsylvania, Philadelphia 19104.
Nowak
P A
PA
Moroney
D A
DA
Morton
T E
TE
Jackson
J R
JR
Ehrenkaufer
R L
RL
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
D005462:Fluorine Radioisotopes; D008024:Ligands; D009578:Nitrobenzenes; D017448:Receptors, Dopamine D2; C081030:N-(4-nitrobenzyl)spiperone; D013134:Spiperone; C039167:3-N-methylspiperone