Structure-based design of a novel third-generation antipsychotic drug lead with potential antidepressant properties

Partial agonist activity at the dopamine D 2 receptor (DRD2) is a key feature of third-generation antipsychotics (TGAs). However, TGAs also act as antagonists or weak partial agonists to the serotonin (5-hydroxytryptamine; 5-HT) 2A receptor (5-HT 2A R). Here we present the crystal structures of arip...

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Veröffentlicht in:	Nature neuroscience 2022-01, Vol.25 (1), p.39-49
Hauptverfasser:	Chen, Zhangcheng, Fan, Luyu, Wang, Huan, Yu, Jing, Lu, Dengyu, Qi, Jianzhong, Nie, Fen, Luo, Zhipu, Liu, Zhen, Cheng, Jianjun, Wang, Sheng
Format:	Artikel
Sprache:	eng
Schlagworte:	631/92 692/699/476/1799 Agonists Animal Genetics and Genomics Animal models Animals Antagonists Antidepressants Antidepressive Agents - pharmacology Antipsychotic Agents - pharmacology Antipsychotics Aripiprazole Behavioral Sciences Binding Biological Techniques Biomedical and Life Sciences Biomedicine Cognition Cognitive ability Crystal structure Design Dopamine Dopamine D2 receptors Drug development Mice Neurobiology Neurosciences Pharmacology Pharmacophores Psychotropic drugs Receptors Serotonin Serotonin - metabolism Serotonin S1 receptors Serotonin S2 receptors Side effects
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