tcsc5980 YL0919

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 receptor

IC50:1.78±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]