扎普司特

扎普司特用途

Zaprinast (M&B 22948) 是一种 cGMP 选择性的磷酸二酯酶 (PDE) 抑制剂。Zaprinast 是一种 GPR35 激动剂,对大鼠 GPR35 有很强的激活作用,对人 GPR35 有一定的激活作用。Zaprinast 能通过抗增殖和促凋亡作用减少血管重构。

扎普司特名称

[ CAS 号 ]:
37762-06-4

[ 中文名 ]:
1,4-二氢-5-(2-丙氧基苯基)-7H-1,2,3-三氮(4,5-d)嘧啶-7-酮

[ 英文名 ]:
Zaprinast

[中文别名 ]:

[英文别名 ]:

2-(2-PROPYLOXYPHENYL)-8-AZAPURIN-6-ONE
2-o-propoxyphenyl-8-azapurin-6-one
EINECS 253-655-1
Potassium phosphate monobasic
Zaprinast
3,6-dihydro-5-(2-propoxyphenyl)
Phenylaza purinon
2-(2-Propoxyphenyl)-8-azahypoxanthine
MFCD00214073
B 22,948

扎普司特生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> 代谢酶/蛋白酶 >> 磷酸二酯酶(PDE)

信号通路 >> G 蛋白偶联受体/G 蛋白 >> CXCR

信号通路 >> 免疫及炎症 >> CXCR

研究领域 >> 神经疾病

[ 靶点 ]

PDE[1], GPR35[2]

[参考文献]

[1]. Choi SH , et al. Zaprinast, an inhibitor of cGMP-selective phosphodiesterases, enhances the secretion of TNF-alpha and IL-1beta and the expression of iNOS and MHC class II molecules in rat microglial cells. J Neurosci Res. 2002 Feb 1;67(3):411-21.

[2]. Taniguchi Y, et al. Zaprinast, a well-known cyclic guanosine monophosphate-specific phosphodiesterase inhibitor, is an agonist for GPR35. FEBS Lett. 2006 Sep 18;580(21):5003-8. Epub 2006 Aug 17.

[3]. Keswani AN , et al The cyclic GMP modulators YC-1 and zaprinast reduce vessel remodeling through antiproliferative and proapoptotic effects. J Cardiovasc Pharmacol Ther. 2009 Jun;14(2):116-24.

扎普司特物理化学性质

[ 密度 ]:
1.484g/cm3

[ 沸点 ]:
406.3±47.0 °C at 760 mmHg

[ 熔点 ]:
237-238ºC dec.

[ 分子式 ]:
C₁₃H₁₃N₅O₂

[ 分子量 ]:
271.275

[ 闪点 ]:
199.5±29.3 °C

[ 精确质量 ]:
271.106934

[ PSA ]:
96.55000

[ LogP ]:
0.17

[ 外观性状 ]:
白色至灰白色粉末

[ 蒸汽压 ]:
0.0±0.9 mmHg at 25°C

[ 折射率 ]:
1.719

[ 储存条件 ]:
2-8℃

[ 水溶解性 ]:
Soluble to 100 mM in DMSO

扎普司特安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S26;S36

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

[ WGK德国 ]:
3

[ RTECS号 ]:
XZ6157358

扎普司特文献

Metabolomics analysis of metabolic effects of nicotinamide phosphoribosyltransferase (NAMPT) inhibition on human cancer cells.

PLoS ONE 9(12) , e114019, (2014)

Nicotinamide phosphoribosyltransferase (NAMPT) plays an important role in cellular bioenergetics. It is responsible for converting nicotinamide to nicotinamide adenine dinucleotide, an essential molec...

Inhibition of mitochondrial pyruvate transport by zaprinast causes massive accumulation of aspartate at the expense of glutamate in the retina.

J. Biol. Chem. 288(50) , 36129-40, (2013)

Transport of pyruvate into mitochondria by the mitochondrial pyruvate carrier is crucial for complete oxidation of glucose and for biosynthesis of amino acids and lipids. Zaprinast is a well known pho...

GPR35 activation reduces Ca2+ transients and contributes to the kynurenic acid-dependent reduction of synaptic activity at CA3-CA1 synapses.

PLoS ONE 8 , e82180, (2013)

Limited information is available on the brain expression and role of GPR35, a Gi/o coupled receptor activated by kynurenic acid (KYNA). In mouse cultured astrocytes, we detected GPR35 transcript using...

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