Synthesis and preliminary studies of ¹¹C-labeled tetrahydro-1,7-naphthyridine-2-carboxamides for PET imaging of metabotropic glutamate receptor 2.

ABSTRACT: Selective modulation of metabotropic glutamate receptor 2 (mGlu₂) represents a novel therapeutic approach for treating brain disorders, including schizophrenia, depression, Parkinson's disease (PD), Alzheimer's disease (AD), drug abuse and addiction. Imaging mGlu₂ using positron emission tomography (PET) would allow for in vivo quantification under physiological and pathological conditions and facilitate drug discovery by enabling target engagement studies. In this paper, we aimed to develop a novel specific radioligand derived from negative allosteric modulators (NAMs) for PET imaging of mGlu₂. Methods. A focused small molecule library of mGlu₂ NAMs with tetrahydro naphthyridine scaffold was synthesized for pharmacology and physico

SUBMITTER: Zhang X 

PROVIDER: S-EPMC7532674 | biostudies-literature | 2020

REPOSITORIES: biostudies-literature