Indiplon is a potent GABAA receptor positive allosteric modulator that acts at the benzodiazepine site (Ki values are 1.2 and 1.7nM in rat frontal cortex and cerebellum respectively).
信号通路
Transmembrane Transporters
靶点
GABAA receptor
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IC50
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体外研究
Indiplon displays ~ 10-fold selectivity for α1 subunit-containing receptors (EC50 values are 2.6, 24, 60 and 77nM for α1β2γ2, α2β2γ2, α3β3γ2 andα5β2γ2 receptors respectively).
体内研究
Indiplon exhibits sedative, hypnotic, anxiolytic and anticonvulsant activity and is orally active. Indiplon is a novel sedative-hypnotic recently approved for the treatment of insomnia. Indiplon is a novel sedative-hypnotic that modulates subunits of the GABA receptor complex in order to induce sedation. Indiplon shows a higher affinity and selectivity to GABAA receptors.
临床实验
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特征
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相关实验数据(此数据来自于公开文献,信裕生物并不保证其有效性):
酶活性检测实验
方法
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细胞实验
细胞系
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浓度
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处理时间
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方法
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动物实验
动物模型
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配制
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剂量
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给药方式
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参考文献: 1. Lankford A, et al. Neuropsychiatr Dis Treat. 2007 Dec, 3(6), 765-773.
2. Shimizu M, et al. Drug Metab Dispos. 2014 Apr, 42(4), 751-758.
包装清单: