Visualization of Receptor-Interacting Protein Kinase 1 (RIPK1) by Brain Imaging with Positron Emission Tomography.

ABSTRACT: We report the development of the first positron emission tomography (PET) radiotracer, [¹⁸F]CNY-07, based on a highly specific and potent RIPK1 inhibitor, Nec-1s, for RIPK1/necroptosis brain imaging in rodents. [¹⁸F]CNY-07 was synthesized through copper-mediated ¹⁸F-radiolabeling from an aryl boronic ester precursor and studied in vivo PET imaging in rodents. PET imaging results showed that [¹⁸F]CNY-07 can penetrate the blood-brain barrier with a maximum percent injected dose per unit volume of 3 at 10 min postinjection in the brain in vivo. Self-blocking studies of [¹⁸F]CNY-07 by pretreating with unlabeled molecules in rodents showed reduced radioactivity in animal brains (30% radioactivity decreased), indicating the bin

SUBMITTER: Lan Y 

PROVIDER: S-EPMC8858444 | biostudies-literature | 2021 Oct

REPOSITORIES: biostudies-literature