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P2X4 BLOCKADE AS A NEW THERAPEUTICAL STRATEGY TO RELIEVE VISCERAL PAIN IN A RAT MODEL OF COLITIS (Hall A, Poster Hall - Walter E. Washington Convention Center) - Mar 14, 2024 - Abstract #DDW2024DDW_2967; Conclusion. The blockade of P2X4R allows an effective control of visceral hypersensitivity contextually to an anti-inflammatory effect, thus substantiating the concept that the modulation of P2X4R can represent a viable approach for the management of visceral pain associated with inflammatory colitis.
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Preclinical, Journal: Anti-inflammatory Effects of Novel P2X4 Receptor Antagonists, NC-2600 and NP-1815-PX, in a Murine Model of Colitis. (Pubmed Central) - Jun 22, 2022 In THP-1 cells, lipopolysaccharide and ATP upregulated IL-1β release and NLRP3, caspase-1, caspase-5, and caspase-8 activity, but not of caspase-4. These changes were prevented by NC-2600 and NP-1815-PX treatment. For the first time, the above findings show that the selective inhibition of P2X4 receptors represents a viable approach to manage bowel inflammation via the inhibition of NLRP3 inflammasome signaling pathways.
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ANTI-INFLAMMATORY EFFECTS OF NOVEL P2X4 RECEPTOR ANTAGONISTS, NC-2600 AND NP-1815-PX, IN A MURINE MODEL OF COLITIS (Poster Hall - San Diego Convention Center) - Apr 25, 2022 - Abstract #DDW2022DDW_1044; This effect was inhibited upon incubation with NC-2600 and NP-1815-PX. Conclusion s: These findings demonstrated for the first time that the direct and selective inhibition of P2X4 receptors represent a viable approach for the management of bowel inflammation via the inhibition of the canonical and non-canonical NLRP3 inflammasome signaling pathways.
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Review, Journal: Nociceptive signaling of P2X receptors in chronic pain states. (Pubmed Central) - Dec 16, 2021 The phase I study of NC-2600 has been completed, and no serious side effects were reported. The roles played by purinergic receptors in evoking neuropathic pain provide crucial insights into the pathogenesis of neuropathic pain.
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[VIRTUAL] Nippon Chemiphar () - May 31, 2021 - Abstract #BIO2021BIO_447; Although several P2X3R antagonists have been developed, we believe P2X4R is ideal target for chronic cough and NC-2600 will be effective for wider range of chronic cough than targeting P2X3. Its Ph-1 is completed in Japan, and no taste disturbances were observed, which is one of concerns of P2X3R antagonists.
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