Highly potent and selective inhibitor of� glutamate carboxypeptidase 2 (GCP II/N-acetylated α
-linked dipeptidase/NAALADase) with a Ki
value of 275 pM. Neuroprotective; protects against glutamate-mediated motor neuron degeneration and reduces volume of injury following middle cerebral artery occlusion (MCAO).
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Inhibition of glutamate carboxypeptidase II (GCPII) activity as a treatment for cognitive impairment in multiple sclerosis.
Rahn et al.
Proc.Natl.Acad.Sci.U S A (Epub ahead of print], 2012;
Design, synthesis, and biological activity of a potent inhibitor of the neuropeptidase N-acetylated α-linked acidic dipeptidase.
Jackson et al.
Selective inhibition of NAALADase, which converts NAAG to glutamate, reduces ischemic brain injury.
Slusher et al.
NAALADase inhibition protects motor neurons against chronic glutamate toxicity.
Thomas et al.