Traxoprodil mesylate (CP 101606 mesylate) is a potent, selective N-methyl-D-aspartate (NMDA) antagonist with selectivity for the NR2B subunit.
Traxoprodil mesylate potently protects cultured hippocampal neurons from glutamate toxicity (IC50=10 nM), dramatically reduces both the open dwell-time and frequency of channel opening of NR1/NR2B-containing receptors, but only modestly inhibits NR1/NR2A and NR1/NR2C channel activity.
Traxoprodil mesylate exhibits neuroprotective, analgesic, and anti-Parkinsonian effects in animal studies.
