In vitro and in vivo Human Metabolism of (S)-[¹⁸F]Fluspidine - A Radioligand for Imaging σ₁ Receptors With Positron Emission Tomography (PET).

ABSTRACT: (S)-[¹⁸F]fluspidine ((S)-[¹⁸F]1) has recently been explored for positron emission tomography (PET) imaging of sigma-1 receptors in humans. In the current report, we have used plasma samples of healthy volunteers to investigate the radiometabolites of (S)-[¹⁸F]1 and elucidate their structures with LC-MS/MS. For the latter purpose additional in vitro studies were conducted by incubation of (S)-[¹⁸F]1 and (S)-1 with human liver microsomes (HLM). In vitro metabolites were characterized by interpretation of MS/MS fragmentation patterns from collision-induced dissociation or by use of reference compounds. Thereby, structures of corresponding radio-HPLC-detected radiometabolite

SUBMITTER: Ludwig FA 

PROVIDER: S-EPMC6585474 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature