Renovis, Inc. (a wholly-owned subsidiary of Evotec AG), South San Francisco, CA 94080, USA.
Bioorg Med Chem Lett. 2010 Dec 1;20(23):7076-9. doi: 10.1016/j.bmcl.2010.09.099. Epub 2010 Sep 22.
5-Benzyloxytryptamine 19 was found to act as an antagonist of the TRPM8 ion-channel. For example, 19 had an IC(50) of 0.34 μM when menthol was used as the stimulating agonist. Related commercially-available tryptamine derivatives showed diminished, or no antagonist activity at TRPM8. The structural similarity of 5-benzyloxytryptamine to other literature TRPM8 antagonists was noted.
5-苄氧基色胺 19 被发现作为 TRPM8 离子通道的拮抗剂。例如，当薄荷醇被用作刺激激动剂时，19 的 IC（50）为 0.34 μM。相关的市售色胺衍生物在 TRPM8 显示出减弱或没有拮抗活性。注意到 5-苄氧基色胺与其他文献中的 TRPM8 拮抗剂具有结构相似性。
