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]
References:
[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)