(+)-[18F]Flubatine as a novel α4β2 nicotinic acetylcholine receptor PET ligand-results of the first-in-human brain imaging application in patients with β-amyloid PET-confirmed Alzheimer's disease and healthy controls.
Solveig TiepoltGeorg-Alexander BeckerStephan WilkeDiego CecchinMichael RullmannPhilipp M MeyerHenryk BarthelSwen HesseMarianne PattJulia LuthardtGudrun WagenknechtBernhard SattlerWinnie Deuther-ConradFriedrich-Alexander LudwigSteffen FischerHermann-Josef GertzRené SmitsAlexander HoeppingJörg SteinbachPeter BrustOsama SabriPublished in: European journal of nuclear medicine and molecular imaging (2020)
(+)-[18F]Flubatine is a safe and stable PET ligand. Full kinetic modeling can be realized by 1TCM without metabolite correction. (+)-[18F]Flubatine binding affinity was high enough to detect group differences. Of interest, correlation between white matter β-amyloid PET uptake and (+)-[18F]Flubatine binding indicated an association between white matter integrity and availability of α4β2 nAChRs. Overall, (+)-[18F]Flubatine showed favorable characteristics and has therefore the potential to serve as α4β2 nAChR-targeting PET ligand in further clinical trials.