CR4056

CR4056 is a **first-in-class imidazoline-2 (I2) receptor ligand** with potent analgesic activity demonstrated in various preclinical models of chronic, neuropathic, and inflammatory pain, as well as osteoarthritis and postoperative pain. Its mechanism of action primarily involves modulation of imidazoline-2 receptors, inhibition of NMDA receptor-mediated currents (favoring GluN1-GluN2B over GluN1-GluN2A subtypes), and inhibition of PKCε translocation in dorsal root ganglia neurons—all contributing to both analgesic and neuroprotective effects. CR4056 shows selective synergy with opioids (notably morphine) but does not bind opioid receptors. It has also demonstrated beneficial effects on neuroinflammation and cognitive impairment in animal models of Alzheimer's disease.

Other names

2-phenyl-6-(1H-imidazol-1yl) quinazoline