Radiosynthesis and In Vitro Evaluation of [¹¹C]tozadenant as Adenosine A_2A Receptor Radioligand.

ABSTRACT: Tozadenant (4-hydroxy-N-(4-methoxy-7-morpholinobenzo[d]thiazol-2-yl)-4-methylpiperidine-1-carboxamide) is a highly selective adenosine A_2A receptor (A_2AR) antagonist and a promising lead structure for the development of A_2AR-selective positron emission tomography (PET) probes. Although several ¹⁸F-labelled tozadenant derivatives showed favorable in vitro properties, recent in vivo PET studies observed poor brain penetration and lower specific binding than anticipated from the in vitro data. While these findings might be attributable to the structural modification associated with ¹⁸F-labelling, they could also reflect inherent properties of the parent compound. However, PET studies with radioisotopologues of tozadenant to

SUBMITTER: Humpert S 

PROVIDER: S-EPMC10935082 | biostudies-literature | 2024 Feb

REPOSITORIES: biostudies-literature