APotential Fluorine-18LabeledPET Radiotracer for ImagingSigma-1 Receptors in theCNS

A series of brain uptake studies and PET imaging studies were conducted with the r1 selective imaging agent, [ F]FBFPA. The results of the study indicate that this radiotracer readily crosses the blood-brain barrier and labels r1 receptors in vivo. In vivo blocking studies with a r1 selective ligand and a nonselective r1/ r2 receptor ligand indicates that [ F]FBFPA labels r1 and not r2 receptors in rodent brain. PET imaging studies demonstrated a high uptake in regions of rhesus monkey brain having a high density of r1 receptors. The uptake of [ F]FBFPA was displaced by the sigma ligand, haloperidol (1 mg/kg, i.v.). In vivo blocking studies indicate that the progesterone blocked the brain uptake of [F]FBFPA in rat brain. These data indicate that [F]FBFPA is a potential radiotracer for imaging r1 receptors in the CNS in vivo with PET. Synapse 58:267–274, 2005. VC 2005 Wiley-Liss, Inc.

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