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YL0919

SKU: orb1226512

Description

An orally active, dual 5-HT1A agonist and selective serotonin reuptake inhibitor with Ki of 0.19 nM and IC50 of 1.78 nM, respectively; shows no affinity for dopamine receptors and others 5-HT receptors; inhibits forskolin-stimulated cAMP formation and 5-HT uptake in both rat cortical synaptosomes and recombinant cells; significantly reverses the depressive-like behaviors in chronically stressed rats.

Images & Validation

Key Properties

CAS Number1339058-04-6
MW334.8404
Purity>98% (HPLC)
FormulaC18H23ClN2O2
SMILESO=C1C=CC=CN1CC2(O)CCN(CC3=CC=CC=C3)CC2.[H]Cl
Target5-HT Receptor
SolubilityDMSO: ≥ 30 mg/mL

Bioactivity

In Vivo
Hypidone hydrochloride (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. Hypidone hydrochloride (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, Hypidone hydrochloride displays no effect on the locomotor activity in a separate OFT. Furthermore, the antidepressant-like effect of Hypidone hydrochloride in TST and FST is completely bunted by coadministration with WAY-100635. 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.
In Vitro
Hypidone hydrochloride 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. Hypidone hydrochloride (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 Hypidone hydrochloride-mediated inhibition of forskolin-stimulated cAMP formation. Hypidone hydrochloride 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.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

YL-0919 | YL 0919

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Protocol Information

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200 mg
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2 mg
$ 80.00
5 mg
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50 mg
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100 mg
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