Name | YL0919 |
Synonyms | 0919 YL0919 CS-2407 YL0919 (YL-0919 YL0919 hydrochloride Hypidone hydrochloride |
CAS | 1339058-04-6 |
Molecular Formula | C18H23ClN2O2 |
Molar Mass | 334.84 |
Solubility | DMSO: ≥ 30 mg/mL |
Storage Condition | -20℃ |
In vitro study | YL0919 inhibits the uptake of [ 3 H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells stably expressing hSERT with IC 50 values of 1.78 nM and 1.93,respectively.YL0919 (0.01 nM-10 μM) concentration-dependently inhibits forskolin-stimulated cAMP formation, exerts a concentration-dependent inhibitory effect on cAMP formation with an IC 50 of approximately 23.9 nM. And in antagonism studies, WAY-100635prevents YL0919-mediated inhibition of forskolin-stimulated cAMP formation. YL0919 shows affinities to rat 5-HT1Areceptors, SERTs, NETs, and DATs, it binds to 5-HT1Areceptor, serotonin transporter (SERT) with high affinity (K i =0.19 and 0.72 nM, respectively), but its affinity to NET and DAT are low, blocking [ 3 H]nisoxetine and [ 3 H]win35428 binding with Kivalues of 650 nM and 2652 nM respectively. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.986 ml | 14.932 ml | 29.865 ml |
5 mM | 0.597 ml | 2.986 ml | 5.973 ml |
10 mM | 0.299 ml | 1.493 ml | 2.986 ml |
5 mM | 0.06 ml | 0.299 ml | 0.597 ml |
biological activity | YL0919 is an orally active antidepressant with dual activity, is a highly selective 5-HT uptake blocker and potent 5-HT1A receptor agonist (Ki = 0.19 nM). YL0919 inhibited the uptake of [3H]-5-HT in rat cerebral cortex synaptosomes and HEK293 cells, with IC50s of 1.78 nM and 1.93 nM, respectively. YL0919 shows obvious antidepressant effect in animal models, which is of great significance to the study of depression. |
Animal Model: | Male ICR mice weighing 18–22 g |
Dosage: | 1.25, 2.5, and 5 mg/kg |
Administration: | Oral administration |
Result: | Had an effect on Antidepressant-like mice in TST and FST. |