期刊
ACS CHEMICAL NEUROSCIENCE
卷 1, 期 1, 页码 19-24出版社
AMER CHEMICAL SOC
DOI: 10.1021/cn9000186
关键词
Pain; acid-sensing; ion channel; ASIC-3; degenerin
The synthesis, structure activity relationship (SA R), and pharmacological evaluation of analogs of the acid-sensing ion channel (ASIC) inhibitor A-317567 are reported. It was found that the compound with an acetylenic linkage was the most potent ASIC-3 channel blocker. This compound reversed mechanical hypersensitivity in the rat iodoacetate model of osteoarthritis pain, although sedation was noted. Sedation was also observed in ASIC-3 knockout mice, questioning whether sedation and antinociception are mediated via a non-ASIC-3 specific mechanism.
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