Quantification of Cerebral A1 Adenosine Receptors in Humans using [18F]CPFPX and PET

Adenosine is an important neuromodulator. Basic cerebral effects of adenosine are exerted by the A1 adenosine receptor (A1AR), which is accessible in vivo by the novel ligand [18F]8-cyclopentyl-3-(3-fluoropropyl)-1-propylxanthine ([18F]CPFPX) and positron emission tomography (PET). The present study...

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Bibliographic Details
Published in:Journal of cerebral blood flow and metabolism 2004-03, Vol.24 (3), p.323-333
Main Authors: Meyer, Philipp T, Bier, Dirk, Holschbach, Marcus H, Boy, Christian, Olsson, Ray A, Coenen, Heinz H, Zilles, Karl, Bauer, Andreas
Format: Article
Language:English
Subjects:
Adenosine A1 Receptor Antagonists
Adult
Animals
Biological and medical sciences
Cerebral Cortex - diagnostic imaging
Cerebral Cortex - metabolism
Fluorine Radioisotopes - metabolism
Humans
Image Processing, Computer-Assisted
Male
Medical sciences
Neurology
Receptor, Adenosine A1 - metabolism
Statistics as Topic
Tomography, Emission-Computed
Vascular diseases and vascular malformations of the nervous system
Xanthines - metabolism
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Summary:Adenosine is an important neuromodulator. Basic cerebral effects of adenosine are exerted by the A1 adenosine receptor (A1AR), which is accessible in vivo by the novel ligand [18F]8-cyclopentyl-3-(3-fluoropropyl)-1-propylxanthine ([18F]CPFPX) and positron emission tomography (PET). The present study investigates the applicability of kinetic models to describe the cerebral kinetics of [18F]CPFPX in order to quantify A1AR density in vivo. Six healthy volunteers underwent dynamic PET scanning and arterial blood sampling after bolus injection of [18F]CPFPX. For quantitative analysis, a standard two-tissue compartment model (2TCM) was compared with a one-tissue compartment model (1TCM) and Logan's graphical analysis (GA). The 2TCM described the cerebral kinetics of [18F]CPFPX significantly better than the 1TCM (in all regions and subjects examined). The estimated values of the regional total distribution volumes (DVt) correlated strongly between the 2TCM and GA (linear regression r2 = 0.99, slope: 1.007). The DVt correlation between the 2TCM and the 1TCM was comparably high, but there was a significant bias towards lower DVt estimates given by the 1TCM (r2: 0.99, slope: 0.929). It is concluded that a 2TCM satisfactorily accounts for the cerebral kinetics of [18F]CPFPX. GA represents an attractive alternative method of analysis.
ISSN:0271-678X
1559-7016
DOI:10.1097/01.WCB.0000110531.48786.9D