CS-2407

CS-2407

中文名称CS-2407
中文同义词1-((4-羟基-1-(苯基甲基)-4-哌啶基)甲基)-2(1H)-吡啶酮盐酸盐;化合物YL0919
英文名称YL 0919
英文同义词YL0919 hydrochloride;CS-2407;YL0919 (YL-0919;0919;Hypidone hydrochloride;Inhibitor,5-hydroxytryptamine Receptor,Serotonin Receptor,5-HT Receptor,Hypidone,Hypidone hydrochloride,YL 0919,inhibit,YL-0919;1-((1-Benzyl-4-hydroxypiperidin-4-yl)methyl)pyridin-2(1H)-one hydrochloride
CAS号1339058-04-6
分子式C18H23ClN2O2
分子量334.84
EINECS号
相关类别抑制剂
Mol文件1339058-04-6.mol
结构式CS-2407 结构式

CS-2407 性质

储存条件Store at -20°C
溶解度二甲基亚砜:≥30mg/mL(89.60mM)
形态固体
颜色白色至米白色

CS-2407 用途与合成方法

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。

5-HT 1A Receptor

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: 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.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/11/08HY-100769CS-2407
Hypidone hydrochloride
1339058-04-62 mg500元
2024/11/08HY-100769CS-2407
Hypidone hydrochloride
1339058-04-65 mg800元

CS-2407 上下游产品信息

"CS-2407"相关产品信息
YKL-5-124 yk11 YK4-279 YKL06-061 4-(苯并[D]噻唑-2-基)-2-甲氧基苯酚
主页 | 企业会员服务 | 广告业务 | 联系我们 | 旧版入口 | 中文MSDS | CAS Index | 常用化学品CAS列表 | 化工产品目录 | 新产品列表 | 评选活动 | HS海关编码 | MSDS查询 | 化工站点

Copyright © 2016-2023 ChemicalBook 版权所有  京ICP备07040585号  京公海网安备11010802032676号  

互联网增值电信业务经营许可证:京ICP证150597号  互联网药品信息服务资格证编号(京)-非经营性-2015-0073  信息系统安全等级保护备案证明(三级)  营业执照公示

根据相关法律法规和本站规定,单位或个人购买相关危险物品应取得有效的资质、资格条件。
参考《应急管理部等多部门关于加强互联网销售危险化学品安全管理的通知 (应急〔2022〕119号)》《互联网危险物品信息发布管理规定》