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YL0919

CAS No. : 1339058-04-6

MCE 站：YL0919

产品活性：YL0919 是一种口服活性抗抑郁剂，具有双重活性，是一种高选择性的 5-HT uptake 阻滞剂和有效的 5-HT_1A receptor 激动剂 (K_i=0.19 nM)。YL0919 对大鼠大脑皮层突触体和 HEK293 细胞摄取 [³H]-5-HT 有抑制作用，IC₅₀s 分别为 1.78 nM 和 1.93 nM。YL0919 在动物模型中表现出明显的抗抑郁作用，对抑郁症的研究具有重要意义。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor

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 (K_i=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.

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