What is it about?
CR4056 is an analgesic drug candidate with a novel mechanism of action, acting as a ligand for the imidazoline receptor I2. It showed promising results in animal studies against various types of pain and, more importantly, in patients affected by osteoarthritis. In this paper we have demonstrated a new molecular mode of action.
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Why is it important?
CR4056 exerts its action on neurons involved in the transmission of painful sensations by inhibiting a the translocation to the cell membrane of a kinase heavily involved in nociception. This effect is long lasting and could explain the analgesic effectiveness of this candidate drug.
Perspectives
This mode of action could be shared by other imidazoline ligands, helping in understanding their peculiar pharmacology in counteracting pain, drug addiction and neurodegenerative disorders.
dr gianfranco caselli
Rottapharm Biotech
Read the Original
This page is a summary of: CR4056, a powerful analgesic imidazoline‐2 receptor ligand, inhibits the inflammation‐induced PKCε phosphorylation and membrane translocation in sensory neurons, Bone Marrow Transplantation, August 2019, Wiley,
DOI: 10.1111/bph.14845.
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