Structure-based discovery of nonhallucinogenic psychedelic analogs

@article{Cao2022StructurebasedDO,
  title={Structure-based discovery of nonhallucinogenic psychedelic analogs},
  author={Dongmei Cao and Jing Yu and Huan Wang and Zhipu Luo and Xinyu Liu and Licong He and Jianzhong Qi and Luyu Fan and Lingjie Tang and Zhangcheng Chen and Jinsong Li and Jianjun Cheng and Sheng Wang},
  journal={Science},
  year={2022},
  volume={375},
  pages={403 - 411}
}
Drugs that target the human serotonin 2A receptor (5-HT2AR) are used to treat neuropsychiatric diseases; however, many have hallucinogenic effects, hampering their use. Here, we present structures of 5-HT2AR complexed with the psychedelic drugs psilocin (the active metabolite of psilocybin) and d-lysergic acid diethylamide (LSD), as well as the endogenous neurotransmitter serotonin and the nonhallucinogenic psychedelic analog lisuride. Serotonin and psilocin display a second binding mode in… 

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