309711-59-9

NS 383 is an ASIC blocker. Inhibition was observed at heteromeric ASIC channels. It attenuates pathophysiological nociceptive behaviors in CFA-inflamed and CCI rats.

NS383 is a potent and uniquely selective inhibitor of rat ASICs containing 1a and/or 3 subunits. NS383 inhibits H(+)-activated currents recorded from rat homomeric ASIC1a, ASIC3, and heteromeric ASIC1a+3 with IC50 values ranging from 0.61 to 2.2 μM. NS383 is well tolerated and capable of reversing pathological painlike behaviors, presumably via peripheral actions, but possibly also via actions within central pain circuits[1].

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[1] Munro G, et al. NS383 Selectively Inhibits Acid-Sensing Ion Channels Containing 1a and 3 Subunits to Reverse Inflammatory and Neuropathic Hyperalgesia in Rats. CNS Neurosci Ther. 2016;22(2):135-145. DOI:10.1111/cns.12487