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2-(2-呋喃基)-7-(2-苯基乙基)-7H-吡唑并[4,3-e][1,2,4]噻唑并[1,5-c]嘧啶-5-胺

用途

SCH58261是adenosine A2A receptor竞争性的拮抗剂。

名称

[ CAS 号 ]:
160098-96-4

[ 中文名 ]:
2-(2-呋喃基)-7-(2-苯基乙基)-7H-吡唑并[4,3-e][1,2,4]噻唑并[1,5-c]嘧啶-5-胺

[ 英文名 ]:
SCH 58261

[英文别名 ]:

SCH58261
SCH 58261

生物活性

[ 描述 ]:

SCH58261是adenosine A2A receptor竞争性的拮抗剂。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 腺苷受体

研究领域 >> 癌症

[参考文献]

[1]. Paul A. Beavis et al. Blockade of A2A receptors potently suppresses the metastasis of CD73+ tumors. Proc Natl Acad Sci U S A, 2013 Sep 3, 110(36): 14711-14716.

[2]. Alessia Melani et al. Time-course of protection by the selective A2Areceptor antagonist SCH58261 after transient focal cerebral ischemia. Neurological Sciences, August 2015, Volume 36, Issue 8, pp 1441-1448.

[3]. Varani K et al. Pharmacological and biochemical characterization of purified A2a adenosine receptors in human platelet membranes by [3H]-CGS 21680 binding. Br J Pharmacol, 1996 Apr;117(8):1693-701.

[相关活性小分子]

物理化学性质

[ 密度 ]:
1.54g/cm3

[ 分子式 ]:
C₁₈H₁₅N₇O

[ 分子量 ]:
345.35800

[ 精确质量 ]:
345.13400

[ PSA ]:
100.06000

[ LogP ]:
3.14010

[ 折射率 ]:
1.807

[ 储存条件 ]:
2-8°C

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

[ 海关编码 ]:
2934999090

合成路线

详细合成路线

上下游产品

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海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

文献

On the role of adenosine (A)₂A receptors in cocaine-induced reward: a pharmacological and neurochemical analysis in rats.

Psychopharmacol. Ser. 232(2) , 421-35, (2015)

Several studies have suggested the inhibitory control of adenosine (A)2A receptor stimulation in cocaine-induced behavioral actions.A combination of systemic or local drug injections and in vivo neuro...

Endothelial dysfunction impairs vascular neurotransmission in tail arteries.

Neurochem. Int. 80 , 7-13, (2015)

The present study intends to clarify if endothelium dysfunction impairs vascular sympathetic neurotransmission. Electrically-evoked tritium overflow (100 pulses/5 Hz) was evaluated in arteries (intact...

Adenosine A2AR blockade prevents neuroinflammation-induced death of retinal ganglion cells caused by elevated pressure.

J. Neuroinflammation 12 , 115, (2015)

Elevated intraocular pressure (IOP) is a major risk factor for glaucoma, a degenerative disease characterized by the loss of retinal ganglion cells (RGCs). There is clinical and experimental evidence ...

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