8-(3-Chlorostyryl)caffeine

8-(3-Chlorostyryl)caffeine用途

(E) -8-(3-氯苯乙烯基)咖啡因是一种选择性腺苷A2A受体拮抗剂。(E) -8-(3-氯苯乙烯基)咖啡因通过独立于其对A2A受体的作用的途径抑制Ki值为70 nM的单胺氧化酶B(MAO-B)。(E) -8-(3-氯苯乙烯基)咖啡因有可能用于帕金森病研究[1]。
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8-(3-Chlorostyryl)caffeine名称

[ CAS 号 ]:
147700-11-6

[ 英文名 ]:
8-(3-Chlorostyryl)caffeine

[英文别名 ]:

8-(3-Chlorostyryl)caffeine生物活性

[ 描述 ]:

(E) -8-(3-氯苯乙烯基)咖啡因是一种选择性腺苷A2A受体拮抗剂。(E) -8-(3-氯苯乙烯基)咖啡因通过独立于其对A2A受体的作用的途径抑制Ki值为70 nM的单胺氧化酶B(MAO-B)。(E) -8-(3-氯苯乙烯基)咖啡因有可能用于帕金森病研究[1]。

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> 单胺氧化酶
研究领域 >> 神经疾病
信号通路 >> G 蛋白偶联受体/G 蛋白 >> 腺苷受体

[ 靶点 ]

A2AR

MAO-B:70 nM (Ki)


[参考文献]

[1]. Nevil Vlok, et al. Inhibition of monoamine oxidase B by analogues of the adenosine A2A receptor antagonist (E)-8-(3-chlorostyryl)caffeine (CSC). Bioorg Med Chem. 2006 May 15;14(10):3512-21.

8-(3-Chlorostyryl)caffeine物理化学性质

[ 密度 ]:
1.36g/cm3

[ 沸点 ]:
559.4ºC at 760 mmHg

[ 分子式 ]:
C16H15ClN4O2

[ 分子量 ]:
330.76900

[ 闪点 ]:
292.1ºC

[ 精确质量 ]:
330.08800

[ PSA ]:
61.82000

[ LogP ]:
1.79450

[ 蒸汽压 ]:
1.52E-12mmHg at 25°C

[ 折射率 ]:
1.656

8-(3-Chlorostyryl)caffeine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

8-(3-Chlorostyryl)caffeine文献

Decreased extracellular adenosine levels lead to loss of hypoxia-induced neuroprotection after repeated episodes of exposure to hypoxia.

PLoS ONE 8(2) , e57065, (2013)

Achieving a prolonged neuroprotective state following transient ischemic attacks (TIAs) is likely to effectively reduce the brain damage and neurological dysfunction associated with recurrent stroke. ...

Effect of adenosine A(2A) receptor antagonists and L-DOPA on hydroxyl radical, glutamate and dopamine in the striatum of 6-OHDA-treated rats.

Neurotox. Res. 21 , 222-30, (2011)

A(2A) adenosine receptor antagonists have been proposed as a new therapy of PD. Since oxidative stress plays an important role in the pathogenesis of PD, we studied the effect of the selective A(2A) a...

Vinegar intake enhances flow-mediated vasodilatation via upregulation of endothelial nitric oxide synthase activity.

Biosci. Biotechnol. Biochem. 74 , 1055-61, (2010)

This study examined the effect of acetate on endothelial nitric oxide synthase (eNOS) in human umbilical vein endothelial cells (HUVECs) by immunoblotting assay and the ability of acetic acid to upreg...


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