| First Author | Varlow C | Year | 2020 |
| Journal | Molecules | Volume | 25 |
| Issue | 4 | PubMed ID | 32098347 |
| Mgi Jnum | J:298454 | Mgi Id | MGI:6480135 |
| Doi | 10.3390/molecules25040982 | Citation | Varlow C, et al. (2020) Revisiting the Radiosynthesis of [(18)F]FPEB and Preliminary PET Imaging in a Mouse Model of Alzheimer's Disease. Molecules 25(4) |
| abstractText | [(18)F]FPEB is a positron emission tomography (PET) radiopharmaceutical used for imaging the abundance and distribution of mGluR5 in the central nervous system (CNS). Efficient radiolabeling of the aromatic ring of [(18)F]FPEB has been an ongoing challenge. Herein, five metal-free precursors for the radiofluorination of [(18)F]FPEB were compared, namely, a chloro-, nitro-, sulfonium salt, and two spirocyclic iodonium ylide (SCIDY) precursors bearing a cyclopentyl (SPI5) and a new adamantyl (SPIAd) auxiliary. The chloro- and nitro-precursors resulted in a low radiochemical yield (<10% RCY), whereas both SCIDY precursors and the sulfonium salt precursor produced [(18)F]FPEB in the highest RCYs of 25% and 36%, respectively. Preliminary PET/CT imaging studies with [(18)F]FPEB were conducted in a transgenic model of Alzheimer's Disease (AD) using B6C3-Tg(APPswe,PSEN1dE9)85Dbo/J (APP/PS1) mice, and data were compared with age-matched wild-type (WT) B6C3F1/J control mice. In APP/PS1 mice, whole brain distribution at 5 min post-injection showed a slightly higher uptake (SUV = 4.8 +/- 0.4) than in age-matched controls (SUV = 4.0 +/- 0.2). Further studies to explore mGluR5 as an early biomarker for AD are underway. |
