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CR4056, a powerful analgesic imidazoline‐2 receptor ligand, inhibits the inflammation‐induced PKCε phosphorylation and membrane translocation in sensory neurons

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CR4056 is a first‐in‐class imidazoline‐2 (I2) receptor ligand characterized by potent analgesic activity in different experimental animal models of pain. In a recent phase II clinical trial, CR4056 effectively reduced… Click to show full abstract

CR4056 is a first‐in‐class imidazoline‐2 (I2) receptor ligand characterized by potent analgesic activity in different experimental animal models of pain. In a recent phase II clinical trial, CR4056 effectively reduced pain in patients with knee osteoarthritis. In the present study, we investigated the effects of CR4056 on PKCε translocation in vitro and on PKCε activation in vivo in dorsal root ganglia (DRG) neurons.

Keywords: cr4056 powerful; translocation; imidazoline receptor; receptor ligand

Journal Title: British Journal of Pharmacology
Year Published: 2019

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