First-in-human PET quantification study of cerebral alpha 4 beta 2*nicotinic acetylcholine receptors using the novel specific radioligand (-)-[F-18]Flubatine

摘要

alpha 4 beta 2* nicotinic receptors (alpha 4 beta 2* nAChRs) could provide a biomarker in neuropsychiatric disorders (e.g., Alzheimer's and Parkinson's diseases, depressive disorders, and nicotine addiction). However, there is a lack of alpha 4 beta 2* nAChR specific PET radioligands with kinetics fast enough to enable quantification of nAChR within a reasonable time frame. Following on from promising preclinical results, the aim of the present study was to evaluate for the first time in humans the novel PET radioligand (-)-[F-18]Flubatine, formerly known as (-)-[F-18]NCFHEB, as a tool for alpha 4 beta 2* nAChR imaging and in vivo quantification.'