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There are only 2 currently available radioligands, 2-(18)F-FA and 6-(18)F-FA, for quantitative PET of the main cerebral subtype of nicotinic acetylcholine receptors (α4β2-nAChRs) in humans. Both exhibit slow distribution kinetics in the brain and require several hours for PET imaging. This makes PET of nAChRs with these radioligands logistically difficult and a serious burden for human subjects. The main purpose of this study was to preclinically evaluate (-)-2-(6-(18)F-fluoro-2,3'-bipyridin-5'-yl)-7-methyl-7-azabicyclo[2.2.1]heptane ((18)F-AZAN), our new radiolabeled antagonist of α4β2-nAChRs, that has high binding potential and rapid brain kinetics in baboons.

PET Imaging of Nicotinic Acetylcholine Receptors in Baboons with 18F-AZAN, a Radioligand with Improved Brain Kinetics

PET Imaging of Nicotinic Acetylcholine Receptors in Baboons with ¹⁸F-AZAN, a Radioligand with Improved Brain Kinetics