PET Imaging of Adenosine A1 Receptor Occupancy

PET imaging of adenosine A1 receptor occupancy.

Use of 11C-MPDX and PET to study adenosine A1 receptor occupancy by nonradioactive agonists and antagonists.

UNLABELLED Adenosine A1 receptors (A1Rs) in human and rodent brains can be visualized with the radioligand 8-dicyclopropylmethyl-1-(11)C-methyl-3-propylxanthine ((11)C-MPDX) and PET. Here we investigated whether A1R occupancy by nonradioactive agonists and antagonists can be assessed with this technique. METHODS Small-animal PET scans with arterial blood sampling were obtained for 4 groups of...

Caffeine occupancy of human cerebral A1 adenosine receptors: in vivo quantification with 18F-CPFPX and PET.

UNLABELLED Caffeine is the neuroactive agent in coffee and tea and is a broadly consumed stimulant. It is a nonselective antagonist of the neuromodulator adenosine and, if applied in commonly consumed doses, evokes its stimulating effects through the blockade of adenosine receptors. (18)F-8-cyclopentyl-3-(3-fluoropropyl)-1-propylxanthine ((18)F-CPFPX) has been established as a highly selective ...

PET imaging for receptor occupancy: meditations on calculation and simplification

This invited mini-review briefly summarizes procedures and challenges of measuring receptor occupancy with positron emission tomography. Instead of describing the detailed analytic procedures of in vivo ligand-receptor imaging, the authors provide a pragmatic approach, along with personal perspectives, for conducting positron emission tomography imaging for receptor occupancy, and systematicall...

Selective Inhibitory Effect of Adenosine A1 Receptor Agonists on the Proliferation of Human Tumor Cell Lines

Background: In this study, the effects of three structural analogues of adenosine upon proliferation of human tumor cells were investigated. Previous research showed a cytotoxic effect of adenosine via A3 receptor and A1 receptor and sometimes this effect was receptor independent. The researches showed a differential cytotoxic effect of adenosine and its A3 agonists on cancerous cells, while ot...