| First Author | Hu F | Year | 2021 |
| Journal | Eur J Med Chem | Volume | 213 |
| Pages | 113047 | PubMed ID | 33280897 |
| Mgi Jnum | J:349593 | Mgi Id | MGI:6728321 |
| Doi | 10.1016/j.ejmech.2020.113047 | Citation | Hu F, et al. (2021) (18)F-labeled radiotracers for in vivo imaging of DREADD with positron emission tomography. Eur J Med Chem 213:113047 |
| abstractText | Designer Receptors Exclusively Activated by Designer Drugs (DREADD) are a preclinical chemogenetic approach with clinical potential for various disorders. In vivo visualization of DREADDs has been achieved with positron emission tomography (PET) using (11)C radiotracers. The objective of this study was to develop DREADD radiotracers labeled with (18)F for a longer isotope half-life. A series of non-radioactive fluorinated analogs of clozapine with a wide range of in vitro binding affinities for the hM3Dq and hM4Di DREADD receptors has been synthesized for PET. Compound [(18)F]7b was radiolabeled via a modified (18)F-deoxyfluorination protocol with a commercial ruthenium reagent. [(18)F]7b demonstrated encouraging PET imaging properties in a DREADD hM3Dq transgenic mouse model, whereas the radiotracer uptake in the wild type mouse brain was low. [(18)F]7b is a promising long-lived alternative to the DREADD radiotracers [(11)C]clozapine ([(11)C]CLZ) and [(11)C]deschloroclozapine ([(11)C]DCZ). |
