Renovis, Inc. (a wholly-owned subsidiary of Evotec AG), Two Corporate Drive, South San Francisco, CA 94080, USA.
Bioorg Med Chem Lett. 2010 Jan 1;20(1):276-9. doi: 10.1016/j.bmcl.2009.10.113. Epub 2009 Oct 30.
AP18 1 was recently disclosed as an antagonist of the TRPA1 receptor by the research group of Patapoutian. However, no detailed structure-activity relationships around 1 have been disclosed. Thus, a small number of oximes related to AP18 were examined in order to characterize the determinants of TRPA1 activity. Congeners of AP18 were found to possess both agonist and antagonist activity, suggesting that AP18 may behave as a covalent antagonist of the TRPA1 ion-channel.
AP18 1 最近被 Patapoutian 研究团队披露为 TRPA1 受体的拮抗剂。然而，目前尚未公开 1 周围的详细构效关系。因此，研究人员检查了少量与 AP18 相关的肟，以确定 TRPA1 活性的决定因素。发现 AP18 的同系物具有激动剂和拮抗剂活性，这表明 AP18 可能表现为 TRPA1 离子通道的共价拮抗剂。
