Synthesis, Structure−Activity Relationship, and Pharmacological Profile of Analogs of The ASIC-3 Inhibitor A-317567
Year: 2009
Type: article
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.
Source: ACS Chemical Neuroscience
DOI: 10.1021/cn9000186
Institution: Merck & Co., Inc., Rahway, NJ, USA (United States)
Language: English
Topic: Ion Channels and Receptors
Subfield: Sensory Systems
Field: Neuroscience
Domain: Life Sciences
Open Access status: green
OpenAlex ID: W2017276387