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对乙酰氨基酚葡糖苷酸

对乙酰氨基酚葡糖苷酸用途

对乙酰氨基酚葡糖苷酸(APAP-glu)是对乙酰氨基酚(HY-66005)的非活性葡糖苷酸代谢物[1][2]。对乙酰氨基酚是一种选择性环氧合酶-2(COX-2)抑制剂和一种有效的肝脏N-乙酰转移酶2(NAT2)抑制剂[3][4]。

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对乙酰氨基酚葡糖苷酸名称

[ CAS 号 ]:
16110-10-4

[ 中文名 ]:
(4-乙酰氨基苯基)-葡糖苷酸

[ 英文名 ]:
acetaminophen glucuronide

[中文别名 ]:

对乙酰氨基酚葡糖苷酸

[英文别名 ]:

Acetaminophen D-glucuronide
[14C]-Acetaminophen glucuronide
paracetamol glucuronide
acetaminophen glucuronide
acetaminophen O-beta-D-glucosiduronic acid
4-glucuronosido-acetanilide

对乙酰氨基酚葡糖苷酸生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 其他

[体外研究]

对乙酰氨基酚主要通过葡萄糖醛酸化和硫酸化在肝脏代谢,从而产生无毒代谢物对乙酰氨基酚葡萄糖醛酸化物(APAP glu)。对乙酰氨基酚葡萄糖醛酸苷是啮齿动物小管Mrp2和基底外侧Mrp3的底物[1]。

[参考文献]

[1]. Carolina I Ghanem, et al. Shift from biliary to urinary elimination of acetaminophen-glucuronide in acetaminophen-pretreated rats. J Pharmacol Exp Ther. 2005 Dec;315(3):987-95.

[2]. Liudmila L Mazaleuskaya, et al. PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses. Pharmacogenet Genomics. 2015 Aug;25(8):416-26.

[3]. Hinz, B, et al. Acetaminophen (paracetamol) is a selective cyclooxygenase-2 inhibitor in man. FASEB J, 2008. 22(2): p. 383-90.

[4]. Rothen JP, et al. Acetaminophen is an inhibitor of hepatic N-acetyltransferase 2 in vitro and in vivo. Pharmacogenetics. 1998 Dec;8(6):553-9.

对乙酰氨基酚葡糖苷酸物理化学性质

[ 密度 ]:
1.61g/cm3

[ 沸点 ]:
697.4ºC at 760mmHg

[ 分子式 ]:
C₁₄H₁₄D₃NO₈

[ 分子量 ]:
330.30500

[ 闪点 ]:
375.6ºC

[ 精确质量 ]:
330.11400

[ PSA ]:
145.55000

[ 蒸汽压 ]:
2.03E-20mmHg at 25°C

[ 折射率 ]:
1.671

[ 储存条件 ]:
2-8°C

对乙酰氨基酚葡糖苷酸MSDS

对乙酰氨基酚葡糖苷酸安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22

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

[ 海关编码 ]:
29389090

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对乙酰氨基酚葡糖苷酸文献

Simultaneous modelling of the Michaelis-Menten kinetics of paracetamol sulphation and glucuronidation.

Clin. Exp. Pharmacol. Physiol. 36(1) , 35-42, (2009)

1. The aim of the present study was to perform an in vivo estimation of the Michaelis-Menten constants of the major metabolic pathways of paracetamol (APAP). 2. A two-occasion, single-dose cross-over ...

Simultaneous LC-MS/MS quantitation of acetaminophen and its glucuronide and sulfate metabolites in human dried blood spot samples collected by subjects in a pilot clinical study.

Bioanalysis 4(12) , 1429-43, (2012)

In support of a pilot clinical trial using acetaminophen as the model compound to assess dried blood spot (DBS) sampling as the method for clinical pharmacokinetic sample collection, a novel sensitive...

Monitoring paracetamol metabolism after single and repeated administration in pediatric patients with neoplastic diseases.

Int. J. Clin. Pharmacol. Ther. 45(9) , 496-503, (2007)

Paracetamol (PCM) is frequently used in pediatric patients with neoplastic disease. It is metabolized mainly by conjugation, but at therapeutic concentrations, a small fraction of the drug undergoes o...

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