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[11C]-CNS5161
- Development stage
- Discontinued
- Lead developer
- Paion
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Small Molecules
- Administration
- Intravenous
01
Overview
[11C]-CNS5161 is a radiolabeled small molecule designed for use as a Positron Emission Tomography (PET) tracer to image the activated state of the N-methyl-D-aspartate (NMDA) receptor. It is the Carbon-11 labeled version of CNS 5161, a potent and selective non-competitive NMDA receptor antagonist. Unlike tracers that bind to the glutamate or glycine regulatory sites, [11C]-CNS5161 acts as a channel blocker that binds within the ion pore itself in a use-dependent (activity-dependent) manner. This unique property allows researchers to visualize and quantify the open state of the NMDA channel, providing a direct measure of receptor activation rather than just receptor density. Developed originally by CeNeS Pharmaceuticals, the tracer has been utilized in clinical research to investigate glutamatergic dysfunction in various neurological and psychiatric conditions, including neuropathic pain, migraine, and schizophrenia.
- Other names
- (S)-[11C]-1-(2-chloro-5-methylphenyl)-1-methyl-3-(3-pyridyl)guanidine
02
Targets
NMDAR (Glutamate receptor ionotropic, NMDA)
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