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1339058-04-6

中文名稱 CS-2407
英文名稱 YL 0919
CAS 1339058-04-6
更新日期 2024/12/15 19:35:18
分子式 C18H23ClN2O2
分子量 334.84
MOL 文件 1339058-04-6.mol
1339058-04-6 結(jié)構(gòu)式 1339058-04-6 結(jié)構(gòu)式

基本信息

中文別名
化合物YL0919
1-((4-羥基-1-(苯基甲基)-4-哌啶基)甲基)-2(1H)-吡啶酮鹽酸鹽
英文別名
0919
CS-2407
YL0919 (YL-0919
YL0919 hydrochloride

物理化學(xué)性質(zhì)

儲存條件-20°C儲存
溶解度DMSO : ≥ 30 mg/mL (89.60 mM)
形態(tài)Solid
顏色White to off-white
CS-2407價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-100769CS-2407
Hypidone hydrochloride
1339058-04-62 mg500元
2024/11/08HY-100769CS-2407
Hypidone hydrochloride
1339058-04-65 mg800元
2024/11/08HY-100769CS-2407
Hypidone hydrochloride
1339058-04-610 mM * 1 mLin DMSO921元

常見問題列表

生物活性
YL0919 是一種口服活性抗抑郁劑,具有雙重活性,是一種高選擇性的 5-HT uptake 阻滯劑和有效的 5-HT1A receptor 激動劑 (Ki=0.19 nM)。YL0919 對大鼠大腦皮層突觸體和 HEK293 細(xì)胞攝取 [3H]-5-HT 有抑制作用,IC50s 分別為 1.78 nM 和 1.93 nM。YL0919 在動物模型中表現(xiàn)出明顯的抗抑郁作用,對抑郁癥的研究具有重要意義。
靶點

5-HT 1A Receptor

體外研究

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.

體內(nèi)研究

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.
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