CGS-12066 maleate

Names

[ Name ]:
CGS-12066 maleate

[Synonym ]:
7-Trifluoromethyl-4-(4-methyl-1-piperazinyl)pyrrolo-[1,2-a]quinoxaline maleate salt

Biological Activity

[Description]:

CGS-12066 (maleate) is a 5-HT receptor agonist. CGS-12066 has agonist effect for 5-HT1A , 5-HT1B ,5-HT1C and 5-HT1D with pEC50 values of 6.41, 7.56, 4.05 and 7.11, respectively. CGS-12066 can be used for the research of neurological disease[1].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

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].

[In Vitro]

CGS-12066 (maleate) 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[1]。 CGS-12066 (maleate) 对 5-HT1A、5-HT1B、5-HT1C和5-HT1D具有激动作用，pKD 值分别为 7.19、6.94、4.89 和 7.49[1]。 CGS-12066 (maleate) 以低效能刺激肌醇磷酸盐的积累[1]。 CGS-12066 (maleate) 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]。

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₁H₂₁F₃N₄O₄

[ Molecular Weight ]:
450.41

[ Exact Mass ]:
450.15100

[ PSA ]:
98.38000

[ LogP ]:
2.97280

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Articles

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...

Related Compounds

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