内源性四氢异喹啉的脂肪酰酰胺在重组人TRPV1受体上具有活性。
Fatty acyl amides of endogenous tetrahydroisoquinolines are active at the recombinant human TRPV1 receptor.
作者信息
O'Dell David K, Rimmerman Neta, Pickens Sarah R, Walker J Michael
机构信息
The Gill Center for Biomolecular Science, 1101 East Tenth Street, Bloomington, IN 47405, USA.
出版信息
Bioorg Med Chem. 2007 Sep 15;15(18):6164-9. doi: 10.1016/j.bmc.2007.06.032. Epub 2007 Jun 20.
The SAR of capsazepine revealed that tetrahydroisoquinoline (TIQ) moiety is a core pharmacophore of TRPV1 activity. This implied that conjugates of endogenous TIQs with fatty acids would be active at TRPV1 receptors. Six such compounds were synthesized and tested for calcium mobilization at recombinant TRPV1 receptors overexpressed in HEK293 cells. Three compounds showed partial TRPV1 agonism with EC(50) values in the low micromolar range and maximal efficacies between 25% and 55% of capsaicin.
辣椒平的构效关系研究表明，四氢异喹啉（TIQ）部分是TRPV1活性的核心药效基团。这意味着内源性TIQ与脂肪酸的缀合物在TRPV1受体上具有活性。合成了六种此类化合物，并在HEK293细胞中过表达的重组TRPV1受体上测试了它们对钙动员的影响。三种化合物表现出部分TRPV1激动作用，其EC(50)值在低微摩尔范围内，最大效能为辣椒素的25%至55%。
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