KETAMIR-2, a new molecular entity and novel ketamine analog

Ketamir-2 is proposed as a new ketamine analog designed to improve oral bioavailability and to show a better safety profile than existing ketamine treatments. Ketamir-2 is reported as a low-affinity NMDA receptor antagonist that selectively binds to the PCP site, with an IC50 on this site around 100 uM. In receptor and binding selectivity screening, it is described as showing no activity across a broad range of other receptors, transporters, and binding sites. In mice, oral Ketamir-2 is reported not to induce ketamine-like hyperlocomotion. Behavioral pharmacology tests used for anxiolytic and antidepressant effects (Open Field, Elevated Plus Maze, Forced Swimming) are reported to show significant Ketamir-2 effects at variable doses, while ketamine used as a positive control did not consistently differ from vehicle or sometimes showed an opposite response.