CS-2407
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- CAS号:
- 1339058-04-6
- 英文名:
- YL 0919
- 英文别名:
- 0919;CS-2407;YL0919 (YL-0919;YL0919 hydrochloride;Hypidone hydrochloride;Inhibitor,5-hydroxytryptamine Receptor,Serotonin Receptor,5-HT Receptor,Hypidone,Hypidone hydrochloride,YL 0919,inhibit,YL-0919
- 中文名:
- CS-2407
- 中文别名:
- 化合物YL0919;1-((4-羟基-1-(苯基甲基)-4-哌啶基)甲基)-2(1H)-吡啶酮盐酸盐
- CBNumber:
- CB43148080
- 分子式:
- C18H23ClN2O2
- 分子量:
- 334.84
- MOL File:
- 1339058-04-6.mol
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CS-2407化学性质
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储存条件:
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Store at -20°C
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溶解度:
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DMSO : ≥ 30 mg/mL (89.60 mM)
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形态:
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Solid
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颜色:
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White to off-white
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CS-2407性质、用途与生产工艺
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)。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。
YL0919 inhibits the uptake of [
3
H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells stably expressing hSERT with IC
50
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 IC
50
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 [
3
H]nisoxetine and [
3
H]win35428 binding with Ki values of 650 nM and 2652 nM respectively.
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.
Animal Model:
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Male ICR mice weighing 18–22 g
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Dosage:
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1.25, 2.5, and 5 mg/kg
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Administration:
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Oral administration
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Result:
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Had an effect on Antidepressant-like mice in TST and FST.
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CS-2407
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-100769 | CS-2407 Hypidone hydrochloride | 1339058-04-6 | 2 mg | 500元 |
2024/04/30 | HY-100769 | CS-2407 Hypidone hydrochloride | 1339058-04-6 | 5 mg | 800元 |
1339058-04-6, CS-2407 相关搜索:
- 抑制剂
- 化合物YL0919
- 1-((4-羟基-1-(苯基甲基)-4-哌啶基)甲基)-2(1H)-吡啶酮盐酸盐
- 1339058-04-6
- Inhibitor,5-hydroxytryptamine Receptor,Serotonin Receptor,5-HT Receptor,Hypidone,Hypidone hydrochloride,YL 0919,inhibit,YL-0919
- Hypidone hydrochloride
- 0919
- YL0919 (YL-0919
- CS-2407
- YL0919 hydrochloride