cr4056 has been researched along with Inflammation* in 1 studies
1 other study(ies) available for cr4056 and Inflammation
| Article | Year |
|---|---|
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 (I. Effects of CR4056 on bradykinin-induced PKCε translocation were studied in rat sensory neurons by immunocytochemistry. PKCε activation was investigated by immunohistochemistry analysis of DRG from complete Freund's adjuvant-treated animals developing local hyperalgesia. The analgesic activity of CR4056 was tested on the same animals.. CR4056 inhibited PKCε translocation with very rapid and long-lasting activity. CR4056 decreased hyperalgesia and phospho-PKCε immunoreactivity in the DRG neurons innervating the inflamed paw. The effect of CR4056 on PKCε translocation was blocked by pertussis toxin, implying that the intracellular pathways involved G. Our results demonstrate that CR4056 shares the ability to inhibit PKCε translocation with other analgesics. Whether the inhibition of PKCε involves binding to specific subtype(s) of I Topics: Amino Acid Sequence; Analgesics; Animals; Cell Membrane; Cells, Cultured; Dose-Response Relationship, Drug; Freund's Adjuvant; Humans; Imidazoles; Imidazoline Receptors; Inflammation; Male; Pain; Phosphorylation; Protein Kinase C-epsilon; Quinazolines; Rats; Rats, Wistar; Sensory Receptor Cells | 2020 |