4-(4-甲基哌嗪-1-基)-7-(三氟甲基)吡咯并[1,2-a]喹喔啉马来酸盐

用途

CGS-12066(马来酸)是一种5-羟色胺受体激动剂。CGS-12066对5-HT1A、5-HT1B、5-HT1C和5-HT1D具有激动作用,pEC50值分别为6.41、7.56、4.05和7.11。CGS-12066可用于神经系统疾病的研究[1]。

名称

[ CAS 号 ]:
1350965-83-1

[ 中文名 ]:
CGS-12066A马来酸盐

[ 英文名 ]:
CGS-12066 maleate

[英文别名 ]:

生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

[ 靶点 ]

pEC50: 6.41 (5-HT1A), 7.56 (5-HT1B), 4.05 (5-HT1C) and 7.11 (5-HT1D)[1]. pKD: 7.19 (5-HT1A), 6.94 (5-HT1B), 4.89 (5-HT1C) and 7.49 (5-HT1D)[1].

[体外研究]

CGS-12066(马来酸盐)对 5-HT1A、5-HT1B、5-HT1C和 5小时1天具有激动作用,pEC50值分别为 6.41、7.56、4.05和 7.11[1]CGS-12066(马来酸盐)对 5-HT1A、5-HT1B、5-HT1C和5小时1天具有激动作用,pKD基因值分别为 7.19、6.94、4.89和 7.49[1]CGS-12066(马来酸盐)以低效能刺激肌醇磷酸盐的积累[1] CGS-12066(马来酸盐)作为部分激动剂抑制小腿黑质毛喉素刺激的腺苷酸环化酶活性[1]

[参考文献]

[1]. Schoeffter P,et al. Interaction of arylpiperazines with 5-HT1A, 5-HT1B, 5-HT1C and 5-HT1D receptors: do discriminatory 5-HT1B receptor ligands exist?. Naunyn Schmiedebergs Arch Pharmacol. 1989;339(6):675-683.

物理化学性质

[ 分子式 ]:
C₂₁H₂₁F₃N₄O₄

[ 分子量 ]:
450.41

[ 精确质量 ]:
450.15100

[ PSA ]:
98.38000

[ LogP ]:
2.97280

[ 储存条件 ]:
室温

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

文献

Functional consequence of the MET-T1010I polymorphism in breast cancer.

Oncotarget 6(5) , 2604-14, (2015)

Major breast cancer predisposition genes, only account for approximately 30% of high-risk breast cancer families and only explain 15% of breast cancer familial relative risk. The HGF growth factor rec...

Cell-cell adhesions and cell contractility are upregulated upon desmosome disruption.

PLoS ONE 9(7) , e101824, (2014)

Desmosomes are perturbed in a number of disease states - including genetic disorders, autoimmune and bacterial diseases. Here, we report unexpected changes in other cell-cell adhesion structures upon ...

MYC is a critical target of FBXW7.

Oncotarget 6(5) , 3292-305, (2015)

MYC deregulation is a driver of many human cancers. Altering the balance of MYC protein levels at the level of transcription, protein stability, or turnover is sufficient to transform cells to a tumor...

更多文献