Rationalizing the Binding Modes of PET Radiotracers Targeting the Norepinephrine Transporter.

ABSTRACT:

Purpose

A new PET radiotracer ¹⁸F-AF78 showing great potential for clinical application has been reported recently. It belongs to a new generation of phenethylguanidine-based norepinephrine transporter (NET)-targeting radiotracers. Although many efforts have been made to develop NET inhibitors as antidepressants, systemic investigations of the structure-activity relationships (SARs) of NET-targeting radiotracers have rarely been performed.

Methods

Without changing the phenethylguanidine pharmacophore and 3-fluoropropyl moiety that is crucial for easy labeling, six new analogs of ¹⁸F-AF78 with different meta-substituents on the benzene-ring were synthesized and evaluated in a competitive cellular uptake assay and in in vivo animal experiments in r

SUBMITTER: Tutov A 

PROVIDER: S-EPMC9963373 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature