Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HT2C receptor.
Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HT2C receptor.
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DOI：
10.1016/j.bmcl.2018.11.050
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发表时间：
2019-01
影响因子：
2.7
通讯作者：
Yulong Xu;A. Sromek;J. Neumeyer
中科院分区：
文献类型：
--
作者：
Yulong Xu;A. Sromek;J. Neumeyer
合成了一系列新的阿波啡衍生物，对5- ht2受体亚型进行初步筛选。其中，化合物11a和11b被鉴定为对其他5- ht2受体亚型具有高选择性的有效5- ht2基配体。分子对接研究发现，化合物11a11与5- ht2c受体结合位点形成了两个关键相互作用，包括与D3.32的盐桥作用和与N6.55的氢键相互作用。
A series of novel aporphine derivatives were synthesized for initial screening at the 5-HT2receptor subtypes. Among them, Compounds11aand11bwere identified as potent 5-HT2Chit ligands with high selectivity over other 5-HT2receptor subtypes. Molecular docking study revealed that compounds11aand11bformed two key interactions with the binding site of 5-HT2Creceptor, including a salt-bridge to D3.32 and a H-bond interaction with N6.55.