F-DPA

F-DPA (specifically evaluated as the radiolabeled positron emission tomography (PET) tracer [18F]F-DPA) is a novel second-generation pyrazolo[1,5-a]pyrimidine acetamide radioligand that targets the 18 kDa translocator protein (TSPO). TSPO is highly expressed on the outer mitochondrial membrane of activated microglia and macrophages, making it a key biomarker for neuroinflammation and glial activation. Chemically, F-DPA is a fluoroaryl analog of DPA-714, where the fluorine atom is directly linked to the phenyl moiety without an alkyl or alkoxy spacer chain. This direct aryl-fluorine bond provides F-DPA with superior metabolic stability in vivo, resulting in significantly fewer radiolabeled metabolites in the brain and plasma compared to DPA-714. Preclinical studies, primarily conducted by the Turku PET Centre, have demonstrated that [18F]F-DPA has high binding affinity (Ki = 1.7 nM) and selectivity for TSPO, showing promise for imaging neuroinflammation in models of Alzheimer's disease, neuropathic pain, and head and neck squamous cell carcinoma.

Other names

18F-F-DPA18F-FDPA[18F]F-DPA[18F]FDPAN,N-diethyl-2-(2-(4-([18F]fluoro)phenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamideN,N-diethyl-2-(2-(4-[18F]fluorophenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamideN,N-diethyl-2-(2-(4-18F-fluorophenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamideN,N-diethyl-2-(2-(4-fluorophenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamidefluorophenyl-DPA