Parametric Images of the Extrastriatal D2 Receptor Density Obtained Using a High-Affinity Ligand (FLB 457) and a Double-Saturation Method

The potential of positron emission tomography for the quantitative estimation of receptor concentration in extrastriatal regions has been limited in the past because of the low density of the D2 receptor sites in these regions and the insufficient affinity of the most widely used radioligands for do...

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Bibliographic Details
Published in:Journal of cerebral blood flow and metabolism 2001-12, Vol.21 (12), p.1493-1503
Main Authors: Delforge, Jacques, Bottlaender, Michel, Loc'h, Christian, Dolle, Frédéric, Syrota, André
Format: Article
Language:English
Subjects:
Biological and medical sciences
Brain - diagnostic imaging
Brain - metabolism
Cerebellum - chemistry
Cerebellum - diagnostic imaging
Cerebellum - metabolism
Computer Simulation
Corpus Striatum
Dopamine Antagonists
Humans
Investigative techniques, diagnostic techniques (general aspects)
Ligands
Medical sciences
Models, Biological
Nervous system
Pyrrolidines
Radionuclide investigations
Receptors, Dopamine D2 - analysis
Receptors, Dopamine D2 - metabolism
Salicylamides
Temporal Lobe - chemistry
Temporal Lobe - diagnostic imaging
Temporal Lobe - metabolism
Thalamus - chemistry
Thalamus - diagnostic imaging
Thalamus - metabolism
Tomography, Emission-Computed - methods
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Summary:The potential of positron emission tomography for the quantitative estimation of receptor concentration in extrastriatal regions has been limited in the past because of the low density of the D2 receptor sites in these regions and the insufficient affinity of the most widely used radioligands for dopamine receptors. The new method described in this paper permits the estimate of the D2 receptor concentration in the extrastriatal regions using a two-injection protocol and FLB 457, a ligand with a high affinity (20 pmol/L in vitro) with D2 dopamine receptors. This approach is not valid for the striatal regions because some hypotheses cannot be verified (because of the high receptor concentration in these regions). The experimental protocol includes two injections with ligand doses designed to significantly occupy the extrastriatal receptor sites (≈ 90%), while leaving less than 60% of the receptor sites occupied by the ligand in the striatal regions. The results obtained using this double-saturation method are in line with the concentration estimates previously obtained using the multiinjection approach. The receptor concentration is 2.9 ± 0.5 pmol/mL in the thalamus, 1.0 ± 0.2 pmol/mL in the temporal cortex, and 0.35 ± 0.13 pmol/mL in the occipital cortex. This study provides new arguments supporting the presence of a small receptor-site concentration in the cerebellum, estimated at 0.35 ± 0.16 pmol/mL The simplicity of the calculation used to estimate the receptor concentration lends itself easily to parametric imaging. The receptor concentration is estimated pixel by pixel, without filtering. This method permits estimation of the extrastriatal D2 receptor concentration using an experimental protocol that can easily be used in patient studies (i.e., single experiment, no blood sampling, short experiment duration).
ISSN:0271-678X
1559-7016
DOI:10.1097/00004647-200112000-00014