CP-101,606 is an NR2B (
N-methyl D-aspartate receptor subtype 2B) subunit antagonist, that can increase dyskinesia. It reduces Ca
2+/calmodulin-dependent protein kinase II level, at threonine-286 hyperphosphorylation (pCaMKII-Thr286).
[1] It has no effect on the α1-adrenergic receptors.
[2] CP-101,606 has the ability to inhibits the habits, stimulated by cocaine. It also possesses hallucinogenic properties.
[3]CP-101606 mesylate (Traxoprodil mesylate) is a potent noncompetitive antagonist of N-methyl-D-aspartate (NMDA) receptors, selective for the NR2B subunit. CP-101606 mesylate has been shown to be neuroprotective in animal models of brain injury and stroke.