Identification of fluorinated (R)-(−)-aporphine derivatives as potent and selective ligands at serotonin 5-HT2C receptor,Bioorganic & Medicinal Chemistry Letters

当前位置： X-MOL 学术 › Bioorg. Med. Chem. Lett. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Identification of fluorinated (R)-(−)-aporphine derivatives as potent and selective ligands at serotonin 5-HT2C receptor
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2018-11-23 , DOI: 10.1016/j.bmcl.2018.11.050
Yulong Xu , Anna W. Sromek , John L. Neumeyer

A series of novel aporphine derivatives were synthesized for initial screening at the 5-HT₂ receptor subtypes. Among them, Compounds 11a and 11b were identified as potent 5-HT_2C hit ligands with high selectivity over other 5-HT₂ receptor subtypes. Molecular docking study revealed that compounds 11a and 11b formed two key interactions with the binding site of 5-HT_2C receptor, including a salt-bridge to D3.32 and a H-bond interaction with N6.55.

中文翻译：

鉴定氟代（R）-（-）-阿啡吗啡衍生物作为5-羟色胺5-HT _2C受体的有效配体和选择性配体

合成了一系列新颖的阿波啡衍生物，用于5-HT ₂受体亚型的初步筛选。其中，化合物11a和11b被确定为有效的5-HT _2C命中配体，相对于其他5-HT ₂受体亚型具有高选择性。分子对接研究表明，化合物11a和11b与5-HT _2C受体的结合位点形成了两个关键的相互作用，包括与D3.32的盐桥以及与N6.55的H键相互作用。

更新日期：2018-11-23

点击分享查看原文

点击收藏

阅读更多本刊最新论文本刊介绍/投稿指南

全部期刊列表>>