Drug intelligence / Profile preview

[18F]NS12137

Development stage
Preclinical
Lead developer
NeuroSearch
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

[18F]NS12137 is a radiolabeled small molecule ligand designed for positron emission tomography (PET) neuroimaging of the norepinephrine transporter (NET). It serves as a molecular probe to quantify noradrenergic innervation and signaling in the brain. By binding specifically to NET, [18F]NS12137 allows for the non-invasive assessment of noradrenergic system integrity, which is often compromised in neurodegenerative conditions such as Parkinson's disease. Research in animal models, such as the Pink1-/- rat, has demonstrated its utility in identifying reduced NET density in regions like the thalamus and prelimbic area, suggesting its potential as a biomarker for disease progression and therapeutic efficacy in disorders involving noradrenergic dysfunction. The ligand exhibits moderate test-retest reproducibility and high specificity, as evidenced by its displacement by the selective NET inhibitor nisoxetine.

Other names
6-(3-fluoropropyl)-3-(p-tolyl)-8-azabicyclo[3.2.1]oct-2-eneF-18 NS12137F18 NS12137F 18 NS12137
02

Targets

NET (Norepinephrine Transporter)DAT (Dopamine plasma membrane transport protein)SERT (Sodium-dependent serotonin transporter)

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