YL0919

YL0919 (YL0919) 是一种具有双重活性的口服抗抑郁药，作为高度选择性的 5-HT 摄取阻滞剂和有效的 5-HT1Areceptor 激动剂 (Ki=0.19 nM)。

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库存: 现货

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2mg

￥987.00

790.00

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5mg

￥1625.00

1300.00

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10mg

￥2062.00

1650.00

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50mg

￥4850.00

3880.00

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100mg

￥9175.00

7340.00

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Background

YL0919, a novel antidepressant candidate with dual activity as a 5-HT1A receptor agonist and a selective serotonin reuptake inhibitor,the IC50 values of YL-0919 inhibiting the uptake of 5-HT into rat cerebral cortical synaptosomes and human recombinant cells were 1.78±0.34 nM and 1.93±0.18 nM respectively.target: 5-HT1A receptorIC50:1.78±0.34 nM(rat cerebral cortical synaptosomes)IC50:1.93±0.18 nM(human recombinant cells)[1]"In vivo: WAY-100635 completely antagonized the antidepressant-like activity of YL-0919 in both behavioral models, suggesting that activation of the 5-HT1A receptor is critical in the antidepressant-like effect of YL-0919. The administered dose of WAY-100635 ranged from 0.1-0.3 mg/kg, which reportedly has no effect on locomotor activity and only blocks the activation of 5-HT1A receptor.[2]

参考文献:
[1]. Chen, H. X. et al. Antidepressant-like activity of YL-0919: a novel combined selective serotonin reuptake inhibitor and 5-HT1A receptor agonist. PloS one 8, e83271, doi:10.1371/journal.pone.0083271 (2013).
[2]. Qin, J. J. et al. The role of activation of the 5-HT1A receptor and adenylate cyclase in the antidepressant-like effect of YL-0919, a dual 5-HT1A agonist and selective serotonin reuptake inhibitor. Neuroscience letters 582, 104-108, 2014.09.009 (2014)