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We recently demonstrated that (11)C-MePPEP, a PET ligand for CB(1) receptors, has such high uptake in the human brain that it can be imaged for 210 min and that receptor density can be quantified as distribution volume (V(T)) using the gold standard of compartmental modeling. However, (11)C-MePPEP had relatively poor retest and intersubject variabilities, which were likely caused by errors in the measurements of radioligand in plasma at low concentrations by 120 min. We sought to find an analog of (11)C-MePPEP that would provide more accurate plasma measurements. We evaluated several promising analogs in the monkey brain and chose the (18)F-di-deutero fluoromethoxy analog ((18)F-FMPEP-d(2)) to evaluate further in the human brain.

Imaging and Quantitation of Cannabinoid CB1 Receptors in Human and Monkey Brains Using 18F-Labeled Inverse Agonist Radioligands

Imaging and Quantitation of Cannabinoid CB₁ Receptors in Human and Monkey Brains Using ¹⁸F-Labeled Inverse Agonist Radioligands