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Papers of the Week

Papers: 24 Aug 2019 - 30 Aug 2019

Animal Studies, Pharmacology/Drug Development

2020 Jan

Br J Pharmacol



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


Vellani V, Sabatini C, Milia C, Caselli G, Lanza M, Letari O, Rovati L C, Giacomoni C
Br J Pharmacol. 2020 Jan; 177(1):48-64.
PMID: 31454418.


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.