| Literature DB >> 22778804 |
Scott D Kuduk1, Christina N Di Marco, Vera Bodmer-Narkevitch, Sean P Cook, Matthew J Cato, Aneta Jovanovska, Mark O Urban, Michael Leitl, Nova Sain, Annie Liang, Robert H Spencer, Stefanie A Kane, George D Hartman, Mark T Bilodeau.
Abstract
The synthesis, structure-activity relationship (SAR), 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.Entities:
Keywords: ASIC-3; Pain; acid-sensing; degenerin; ion channel
Mesh:
Substances:
Year: 2009 PMID: 22778804 PMCID: PMC3368628 DOI: 10.1021/cn9000186
Source DB: PubMed Journal: ACS Chem Neurosci ISSN: 1948-7193 Impact factor: 4.418