Radiosynthesis and Preclinical Evaluation of [¹⁸F]F-DPA, A Novel Pyrazolo[1,5a]pyrimidine Acetamide TSPO Radioligand, in Healthy Sprague Dawley Rats.

ABSTRACT:

Purpose

Many neurological conditions result in the overexpression of the translocator protein 18 kDa (TSPO), today recognized as a biomarker for microglial activation and neuroinflammation imaging. The pyrazolo[1,5-a]pyrimidine acetamides are a particularly attractive class of TSPO-specific ligands, prompting the development of several positron emission tomography (PET) radiotracers. This includes F-DPA, a recently reported fluorinated ligand (K _i = 1.7 nM), wherein the fluorine atom is directly linked to the phenyl moiety without the presence of an alkyl or alkoxy spacer chain. Reported here is the preparation of [¹⁸F]F-DPA using [¹⁸F]Selectfluor bis(triflate) and the preliminary evaluation of [¹⁸F]F-DPA in healthy rats. Its metabolic pr

SUBMITTER: Keller T 

PROVIDER: S-EPMC5574958 | biostudies-literature | 2017 Oct

REPOSITORIES: biostudies-literature