Novel Agonists of 5HT<sub>2C</sub> Receptors. Synthesis and Biological Evaluation of Substituted 2-(Indol-1-yl)-1-methylethylamines and 2-(Indeno[1,2-<i>b</i>]pyrrol-1-yl)-1-methylethylamines. Improved Therapeutics for Obsessive Compulsive Disorder
作者:Michael Bös、François Jenck、James R. Martin、Jean-Luc Moreau、Andrew J. Sleight、Jürgen Wichmann、Ulrich Widmer
DOI:10.1021/jm970030l
日期:1997.8.1
The syntheses of a series of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2- b]pyrrol-1-yl)-1-methylethylamines are reported. The binding affinities of the compounds at 5HT2C and 5HT2A receptors (79% homology in the transmembrane domain) were determined. The ligands displayed selectivity for 5HT2C receptors relative to 5HT2A receptors. Compounds were functionally characterized both
报道了一系列取代的2-(吲哚-1-基)-1-甲基乙胺和2-(茚并[1,2-b]吡咯-1-基)-1-甲基乙胺的合成。确定了化合物在5HT2C和5HT2A受体上的结合亲和力(跨膜结构域中79%的同源性)。相对于5HT2A受体,配体显示出对5HT2C受体的选择性。化合物在体外和体内均具有5HT2C受体激动剂的功能特征。5f,5l,5n,5o,5q,14c,14f,14k和14m在强迫症动物模型中表现出抗强迫作用。