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

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.

• Publication year

  2020

• Venue

  British Journal of Pharmacology

• Publication date

  2020-01-01

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1111/bph.14845PMID 31454418PMCID PMC6976787
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

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