型号:
产品价格:电议      采购度:1314      原产地:美洲
发布时间:2022/1/21 15:43:22 所属地区:国外 国外
简要描述:
Hypidone hydrochloride (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-HT1A receptor 激动剂 (Ki= nM)。Hypidone hydrochloride 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 nM 和 nM。Hypidone hydrochloride 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
标签:YL0919
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CAS No. : 1339058-04-6
MCE 站:Hypidone hydrochloride
产品活性:Hypidone hydrochloride (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-HT1A receptor 激动剂 (Ki=0.19 nM)。Hypidone hydrochloride 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。Hypidone hydrochloride 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: 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.
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.
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更新时间:2024/1/2 10:19:40
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