Application of Boropinol-B in preparation of medicines for treating insomnia

The invention discloses a new application of a compound Boropinol-B in preparation of medicines for treating insomnia for the first time. Boropinol-B as shown in a formula I acts on a neuron GABAA receptor, and enhances chloride ion internal flow to hyperpolarize nerve cells, thereby achieving centr...

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Bibliographische Detailangaben
Hauptverfasser: LI KANGNING, MU KEMAN, ZHANG DI, ZHANG JIAN, YANG PENG, FENG XINQIAN, MAO SHENGJUN
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a new application of a compound Boropinol-B in preparation of medicines for treating insomnia for the first time. Boropinol-B as shown in a formula I acts on a neuron GABAA receptor, and enhances chloride ion internal flow to hyperpolarize nerve cells, thereby achieving central nervous sedation and inhibiting effects. The Boropinol-B can be used for improving GABA level in the brain by enhancing the activity of GABAergic neurons in a VLPO region in the brain of an insomnia model mouse and thus increasing the release of GABA. The compound has remarkable sedative and hypnotic effects, fast onset of action, quick in-vivo metabolism elimination, short biological half-life period, neither obvious residual effect nor obvious toxic side effects, and is expected to become medicines for treating insomnia with great application prospects. 本发明首次公开了化合物Boropinol-B在制备治疗失眠药物中的新用途。Boropinol-B如式I所示,其作用于神经元GABAA受体,增加氯离子内流使神经细胞超极化,产生中枢神经镇静与抑制作用。其可通过增强失眠模型小鼠脑内VLPO区GABA能神经元的活性,增加GABA的释放从而提高脑内GABA水平。该化合物具有显