[¹⁸F]MK-7246 for Positron Emission Tomography Imaging of the Beta-Cell Surface Marker GPR44.

ABSTRACT: The progressive loss of beta-cell mass is a hallmark of diabetes and has been suggested as a complementary approach to studying the progression of diabetes in contrast to the beta-cell function. Non-invasive nuclear medicinal imaging techniques such as Positron Emission Tomography using radiation emitting tracers have thus been suggested as more viable methodologies to visualize and quantify the beta-cell mass with sufficient sensitivity. The transmembrane G protein-coupled receptor GPR44 has been identified as a biomarker for monitoring beta-cell mass. MK-7246 is a GPR44 antagonist that selectively binds to GPR44 with high affinity and good pharmacokinetic properties. Here, we present the synthesis of MK-7246, radiolabeled with the positron emitter fluorine-18 for preclinical evaluation u

SUBMITTER: Cheung P 

PROVIDER: S-EPMC9962486 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature