Chunk #17 — Adenosine, Receptors and Functions in the CNS — Adenosine A1R and Functions in the CNS — [18F] PET radioligands of adenosine A1R

Source

Purinergic Receptors of the Central Nervous System: Biology, PET Ligands, and Their Applications.

Embedded

yes

Text

In order to improve metabolic stability inherent in [18F]CPFPX, two additional fluorinated PET analogs [18F]CBCPM and [18F]CPMMCB were developed and tested.84 In vitro autoradiographic studies of rat brain slices with [18F]CBCPM and [18F]CPMMCB revealed accumulation of both compounds in regions known to have a high A1R expression. However, in vitro metabolite studies using human liver microsomes identified comparable metabolic instabilities for these radioligands, similar to that of the parent ligand [18F]CPFPX.84