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PMPA (NAALADase inhibitor)
Other Information:
Sold with the permission of AstraZeneca Ltd
Chemical Name:2-(Phosphonomethyl)pentane-1,5-dioic acid
Biological Activity:
Highly potent and selective
inhibitor ofglutamate 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).
Jacksonet
al (1996) Design, synthesis, and biological activity of a potent inhibitor
of the neuropeptidase N-acetylated α-linked acidic dipeptidase. J.Med.Chem. 39
619. Slusheret al (1999) Selective inhibition of NAALADase,
which converts NAAG to glutamate, reduces ischemic brain injury. Nature Med. 5
1396. Thomaset al (2003) NAALADase inhibition protects motor
neurons against chronic glutamate toxicity. Eur.J.Pharmacol. 471
177.
