KETAMIR-2, a new molecular entity and novel ketamine analog.
Frontiers in pharmacology January 1, 2025 Itzchak Angel, Rita Perelroizen, Wendy Deffains et al. 2 citations
Ketamir-2, a new ketamine analog designed for improved oral bioavailability and safety, is a low-affinity NMDA receptor antagonist that selectively binds to the PCP site with an IC50 of about 100 µM. Unlike ketamine, which induces hyperlocomotion in mice—a behavior linked to schizophrenia-like psychomotor agitation—Ketamir-2 does not cause hyperlocomotion. In behavioral tests for anti-depressive and anxiolytic effects (Open Field, Elevated Plus Maze, Forced Swimming Test), Ketamir-2 showed significant effects at variable doses, while ketamine often did not differ from vehicle or showed opposite responses. The findings suggest Ketamir-2 may offer a safer profile without ketamine's dissociative side effects.