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In vivo imaging of adenosine A1 receptors in the human brain with [18F]CPFPX and positron emission tomography.

Abstract：

:The important roles played by the A(1) adenosine receptor (A(1)AR) in brain physiology and pathology make this receptor a target for in vivo imaging. Here we describe the distribution of A(1)ARs in the living human brain with PET, made possible for the first time by the highly potent and selective A(1)AR antagonist 8-cyclopentyl-3-(3-[(18)F]fluoropropyl)-1-propylxanthine ([(18)F]CPFPX). In vivo data demonstrate a rapid cerebral uptake, peaking at 2.9 +/- 0.6% injected dose/liter at 3.3 +/- 1.3 min, followed by a gradual washout. Consistent with the results of autoradiography, high receptor densities occurred in the putamen and the mediodorsal thalamus. Neocortical regions showed regional differences in [(18)F]CPFPX binding, with high accumulation in temporal > occipital > parietal > frontal lobes and a lower level of binding in the sensorimotor cortex. Ligand accumulation was low in cerebellum, midbrain, and brain stem. Metabolism of [(18)F]CPFPX is rapid outside the central nervous system, but the metabolites do not penetrate the blood-brain barrier. In conclusion, in vivo application of [(18)F]CPFPX, a highly potent and selective PET ligand, for the first time allows the imaging of A(1)ARs in the living human brain.

journal_name

Neuroimage

journal_title

NeuroImage

authors

Bauer A,Holschbach MH,Meyer PT,Boy C,Herzog H,Olsson RA,Coenen HH,Zilles K

doi

10.1016/s1053-8119(03)00241-6

keywords:

subject

Has Abstract

pub_date

2003-08-01 00:00:00

pages

1760-9

issue

4

eissn

1053-8119

issn

1095-9572

pii

S1053811903002416

journal_volume

19

pub_type

杂志文章

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