YL0919

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种口服活性双重 5-HT1A 激动剂和选择性血清素再摄取抑制剂，Ki 为 0.19 nM，IC50 为 1.78 nM。

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.

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.

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.

YL-0919 | YL 0919

Endocrinology/Hormones

5-HT Receptor

5-HT| 5-HT1A

Neurological Disease

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1339058-04-6

334.8404

C18H23ClN2O2

>98% (HPLC)

DMSO: ≥ 30 mg/mL

O=C1C=CC=CN1CC2(O)CCN(CC3=CC=CC=C3)CC2.[H]Cl

2(1H)-Pyridinone, 1-[[4-hydroxy-1-(phenylmethyl)-4-piperidinyl]methyl]-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years