elongate the ‘C-terminal part’ of the molecule. Therefore, we were able to explore mimics of the substance P analogs described as inverse agonists. Some compounds presented affinities in the nanomolar range and potent biological activities, while one exhibited a partial inverse agonist behavior similar to a Substance P analog.
                                    在我们先前描述的
1,2,4-三唑上引入第二个手性中心,使我们能够增加多样性并延长分子的“ C端部分”。因此,我们能够探索被称为反向激动剂的P物质类似物的模拟物。一些化合物表现出在纳摩尔范围内的亲和力和强大的
生物活性,而一种则表现出类似于Substance P类似物的部分反向激动剂行为。