Radiofluorinated Analogs of NCS-382 as Potential PET Tracers for Imaging the CaMKIIα Hub Domain.

ABSTRACT: The Ca²⁺/calmodulin-dependent protein kinase II alpha (CaMKIIα) is a key regulator of calcium signaling in the central nervous system and is suggested to play a crucial role in neurodegenerative diseases and stroke. The CaMKIIα hub domain was recently identified as a high-affinity binding site for γ-hydroxybutyric acid (GHB), representing a new target for neurological research and therapy. In this study, we synthesized and evaluated two novel radiofluorinated GHB analogs, [¹⁸F]6 and [¹⁸F]9, to visualize CaMKIIα via this domain in vivo using positron emission tomography (PET). In vitro autoradiography demonstrated specific binding of [¹⁸F]6 to CaMKIIα-rich brain regions, whereas [¹⁸F]9 exhibited apparent nons

SUBMITTER: Sirocchi LS 

PROVIDER: S-EPMC12272552 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature