A series of novel 8-sulfonyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles (THPI) has been synthesized and their ability to interact with 5-HT₆ receptors evaluated in cell-based and radioligand binding assays. Amongst evaluated THPIs, compounds 9.HCl and 20.HCl have been identified as the most potent 5-HT₆ receptor antagonists with K_i values equal to 2.1 nM and 5.7 nM and IC₅₀ values (functional assay) equal to 15 nM and 78 nM, respectively. Affinities of these two compounds for several serotonin receptors in the competitive radioligand binding assays as well as their specificity profiles against a panel of therapeutic targets have been determined.

合成了一系列新型的8-磺酰基取代的2,3,4,5-四氢-1 H-吡啶并[4,3- b ]吲哚（THPI），并评估了它们与5-HT ₆受体相互作用的能力。基于细胞的和放射性配体结合测定。在评估的THPI中，化合物9 .HCl和20 .HCl被确定为最有效的5-HT ₆受体拮抗剂，其K _i值等于2.1 nM和5.7 nM，IC ₅₀值（功能测定）分别等于15 nM和78 nM。在竞争性放射性配体结合测定中，已经确定了这两种化合物对几种血清素受体的亲和力，以及它们对一组治疗靶标的特异性。