YL0919

YL0919 is an orally active antidepressant agent with dual activity as a highly seletive 5-HT uptake blocker and an effective 5-HT1A receptor agonist (Ki=0.19 nM). YL0919 inhibits the uptake of [3H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells with IC50s of 1.78 nM and 1.93 nM, respectively. YL0919 shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder.

Product information

CAS Number: 1339058-04-6

Molecular Weight: 334.84

Formula: C18H23ClN2O2

Chemical Name: 1-[(1-benzyl-4-hydroxypiperidin-4-yl)methyl]-1,2-dihydropyridin-2-one hydrochloride

Smiles: Cl.OC1(CN2C=CC=CC2=O)CCN(CC2C=CC=CC=2)CC1

InChiKey: OXILSFMNCPZGAH-UHFFFAOYSA-N

InChi: InChI=1S/C18H22N2O2.ClH/c21-17-8-4-5-11-20(17)15-18(22)9-12-19(13-10-18)14-16-6-2-1-3-7-16;/h1-8,11,22H,9-10,12-15H2;1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 30 mg/mL (89.60 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

YL0919 inhibits the uptake of [3H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells stably expressing hSERT with IC50 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 IC50 of approximately 23.9 nM. And in antagonism studies, WAY-100635 prevents YL0919-mediated inhibition of forskolin-stimulated cAMP formation. YL0919 shows affinities to rat 5-HT1A receptors, SERTs, NETs, and DATs, it binds to 5-HT1A receptor, serotonin transporter (SERT) with high affinity (Ki=0.19 and 0.72 nM, respectively), but its affinity to NET and DAT are low, blocking [3H]nisoxetine and [3H]win35428 binding with Ki values of 650 nM and 2652 nM respectively.

In Vivo:

YL0919 (oral administration; 1.25 or 5 mg/kg; 4 weeks) and fluoxetine (10 mg/kg) reverses the inhibition of locomotor activity in CUS rats. YL0919 (oral administration; 1.25, 2.5, and 5 mg/kg; 4 weeks) significantly reduces the immobility time in TST in mcie FST in mice. Besides, YL0919 displays no effect on the locomotor activity in a separate OFT. Furthermore, the antidepressant-like effect of YL0919 in TST and FST is completely bunted by coadministration with WAY-100635.

Products are for research use only. Not for human use.