Radiation dosimetry of the α₄β₂ nicotinic receptor ligand (+)-[¹⁸F]flubatine, comparing preclinical PET/MRI and PET/CT to first-in-human PET/CT results.

ABSTRACT:

Background

Both enantiomers of [¹⁸F]flubatine are new radioligands for neuroimaging of α₄β₂ nicotinic acetylcholine receptors with positron emission tomography (PET) exhibiting promising pharmacokinetics which makes them attractive for different clinical questions. In a previous preclinical study, the main advantage of (+)-[¹⁸F]flubatine compared to (-)-[¹⁸F]flubatine was its higher binding affinity suggesting that (+)-[¹⁸F]flubatine might be able to detect also slight reductions of α₄β₂ nAChRs and could be more sensitive than (-)-[¹⁸F]flubatine in early stages of Alzheimer's disease. To support the clinical translation, we investigated a fully image-based internal dosimetry approach

SUBMITTER: Kranz M 

PROVIDER: S-EPMC5074934 | biostudies-literature | 2016 Dec

REPOSITORIES: biostudies-literature