Synthesis and in vivo evaluation of [18F]-N-(p-nitrobenzyl)spiperone ([18F]PNBS) in rats

Nucl Med Biol. 1993 Apr;20(3):269-78. doi: 10.1016/0969-8051(93)90048-y.

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

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Brain / metabolism
  • Chromatography, High Pressure Liquid
  • Fluorine Radioisotopes*
  • Isotope Labeling
  • Ligands
  • Nitrobenzenes / chemical synthesis*
  • Nitrobenzenes / metabolism
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Dopamine D2 / metabolism
  • Spiperone / analogs & derivatives*
  • Spiperone / chemical synthesis
  • Spiperone / metabolism
  • Tissue Distribution
  • Tomography, Emission-Computed

Substances

  • Fluorine Radioisotopes
  • Ligands
  • Nitrobenzenes
  • Receptors, Dopamine D2
  • N-(4-nitrobenzyl)spiperone
  • Spiperone
  • 3-N-methylspiperone