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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


177


1

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

Authors

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.

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.