Potent inhibitor of glutamate carboxypeptidase II and III (GCP II and III/NAAG peptidase/NAALADase) (Ki
values are 0.8 and 23 nM respectively) that inhibits the hydrolysis of NAAG (IC50
= 2.4 nM). Does not directly interact with NMDA or metabotropic glutamate receptors. Reduces neuronal degeneration in a rat model of� traumatic brain injury (TBI) and reduces locomotor activity in the PCP-model of schizophrenia.
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NAAG peptidase inhibition reduces locomotor activity and some stereotypes in the PCP model of schizophrenia via group II mGluR.
Olszewski et al.
NAAG peptidase inhibitors and their potential for diagnosis and therapy.
Zhou et al.
Nat.Rev.Drug Discov., 2005;4:1015
Local administration of N-acetylaspartylglutamate (NAAG) peptidase inhibitors is analgesic in peripheral pain in rats.
Yamamoto et al.