Pharmacological Characterization of [¹⁸F]-FNM and Evaluation of NMDA Receptors Activation in a Rat Brain Injury Model.

ABSTRACT:

Purpose

NMDA receptors (NMDARs) dysfunction plays a central role in the physiopathology of psychiatric and neurodegenerative disorders whose mechanisms are still poorly understood. The development of a PET (positron emission tomography) tracer able to selectively bind to the NMDARs intra-channel PCP site may make it possible to visualize NMDARs in an open and active state. We describe the in vitro pharmacological characterization of [¹⁸F]-fluoroethylnormemantine ([¹⁸F]-FNM) and evaluate its ability to localize activated NMDA receptors in a rat preclinical model of excitotoxicity.

Procedures

The affinity of the non-radioactive analog for the intra-channel PCP site was determined in a radioligand competition assay using [³H]TCP ([³H]

SUBMITTER: Beaurain M 

PROVIDER: S-EPMC10333392 | biostudies-literature | 2023 Aug

REPOSITORIES: biostudies-literature