N-Methyl-D-Aspartate (NMDA) receptor modulators: a patent review (2015-present).

- Supporting evidence shows that subtype-selective NMDA receptor antagonists show an improved safety profile compared to broad-spectrum channel blockers. Although GluN2B-selective antagonists are by far the most extensively investigated subtype-selective modulators, they have shown only modest clinical efficacy so far. To overcome the limitations that have hampered the clinical development of previous subtype-selective NMDA receptor antagonists, future studies with improved animal models that better reflect human NMDA receptor pathophysiology are warranted. The increased availability of subtype-selective probes will allow target engagement studies and proper dose finding in future clinical trials.