Synthesis and Characterization of [¹⁸F]JNJ-46356479 as the First ¹⁸F-Labeled PET Imaging Ligand for Metabotropic Glutamate Receptor 2.

ABSTRACT:

Purpose

Metabotropic glutamate receptor 2 (mGluR2) has been implicated in various psychiatric and neurological disorders, such as schizophrenia and Alzheimer's disease. We have previously developed [¹¹C]7 as a PET radioligand for imaging mGluR2. Herein, [¹⁸F]JNJ-46356479 ([¹⁸F]8) was synthesized and characterized as the first ¹⁸F-labeled mGluR2 imaging ligand to enhance diagnostic approaches for mGluR2-related disorders.

Procedures

JNJ-46356479 (8) was radiolabeled via the copper (I)-mediated radiofluorination of organoborane 9. In vivo PET imaging experiments with [¹⁸F]8 were conducted first in C57BL/6 J mice and Sprague-Dawley rats to obtain whole body biodistribution and brain uptake profile. Subsequent PET studies we

SUBMITTER: Yuan G 

PROVIDER: S-EPMC8277681 | biostudies-literature | 2021 Aug

REPOSITORIES: biostudies-literature