Selective glutamate carboxypeptidase II (GCP II) inhibitor (IC50
= 90 nM). Selective for GCP II over NMDA, kainate and AMPA glutamate receptors and MMP-1, -2, -3, -7, -9, ACE and NEP metalloproteases. Antinociceptive in a rat model of neuropathic pain and protects against motor neuron death in familial amyotrophic lateral sclerosis mice. Orally bioavailable.
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All Tocris products are intended for laboratory research use only.
Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.
Majer et al.
Glutamate carboxypeptidase II inhibition protects motor neurons from death in familial amyotrophic lateral sclerosis models.
Ghadge et al.
Pharmacokinetics and pharmacodynamics of the glutamate carboxypeptidase II inhibitor 2-MPPA show prolonged alleviation of neuropathic pain through an indirect mechanism.
Vornov et al.