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Chem Biol Drug Des. 2017 Mar;89(3):353-364. doi: 10.1111/cbdd.12843. Epub 2016 Sep 26.

Synthesis and biological evaluation of novel flavanone derivatives as potential antipsychotic agents.

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Department of Pharmacology, Xuanwu Hospital of Capital Medical University, Beijing Institute for Brain Disorders, Beijing Engineering Research Center for Nerve System Drugs, Key Laboratory for Neurodegenerative Diseases of Ministry of Education, Beijing, China.
School of Chemical Biology and Pharmaceutical Sciences, Capital Medical University, Beijing, China.


In this study, a series of novel flavanone derivatives were designed and synthesized, and the antipsychotic activities of the target compounds were evaluated in vitro and in vivo. The results showed that synthesized compounds 7a-7g decreased the activity of dopamine D2 receptors in HEK293 cells co-transfected with D2 receptor/G protein α16a, with IC50 values of 0.051-0.35 μm. Compounds 7a-7g inhibited the over-production of nitric oxide stimulated by lipopolysaccharide/interferon-γ in BV-2 microglial cells. In mice, intragastric administration of 7d, 7e, and 7g reversed the increase in locomotor activity induced by MK-801 (an antagonist of NMDA receptors) and decreased the hyperactivity of climbing behavior induced by apomorphine (a dopamine receptor agonist). These results suggest that some of the novel flavanone derivatives have potential antipsychotic effects and may be useful in the treatment of schizophrenia.


MK-801; Neuroinflammation; apomorphine; dopamine D2 receptor; flavanone derivatives; schizophrenia

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