The quest for novel treatments for chronic pain and inflammation continues to be an area of intense research.   Under conditions of acidosis, tissue damage can often result leading to acute or chronic pain.  A number of receptors and ion channels expressed in neurons have been shown to be modulated by protons.  Among them, the acid-sensing ion channel-3 (ASIC3) is representative of a proton-gated subgroup of degenerin/epithelial Na+ cation channel family.  There is substantial evidence that ASIC3 serves as a pH sensor playing an important role in conveying the pain sensation resulting from tissue acidosis.  Accordingly, small molecule inhibitors of the ASIC3 channels are of considerable interest to study the physiological role of ASIC3.  In this paper, the synthesis, SAR, and pharmacological evaluation of analogs of the ASIC channel inhibitor A-317567 are reported.

Synthesis, SAR, and pharmacological profile of analogs of the ASIC-3 inhibitor A-317567

239th National Meeting (2010)

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