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4-羟基-1,5-二甲基-2-苯基-1,2-二氢-3H-吡唑-3-酮

用途

4-羟基安替比林(4-羟基苯那酮；NSC 174055)是安替比灵(HY-B0171)的主要代谢产物,可作为生物分布启动子。4-羟基安替比林可增加胞磷胆碱和安替比灵在脑内的浓度比分布[1][2]。

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名称

[ CAS 号 ]:
1672-63-5

[ 中文名 ]:
4-羟基安替比林

[ 英文名 ]:
4-hydroxyantipyrine

[英文别名 ]:

MFCD00003143
1-phenyl-2,3-dimethyl-4-hydroxy-pyrazoline-5-on
4-Hydroxy-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one
1-Phenyl-2,3-dimethyl-4-hydroxy-5-pyrazolone
Prestwick_270
hydroxy-4 antipyrine
Antipyrine,4-hydroxy
4-Hydroxyantipyrine

生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 其他

信号通路 >> 其他 >> 其他

[体外研究]

4-羟基安替比林增加脑和肝中胞磷胆碱的组织-血浆浓度比,以及脑、肝和心脏中硫喷妥钠的组织-血液浓度比[1]。4-羟基安替比林增强了安替比因的血脑屏障(BBB)通透性,考虑到与脑中安替比灵的Kp值增加有关[2]。

[参考文献]

[1]. Ohkawa Y, et al. Effects of 4-hydroxyantipyrine and its 4-O-sulfate on antipyrine as biodistribution promoter. Biol Pharm Bull. 2001 May;24(5):529-34.

[2]. Ohkawa Y, et al. Application of 4-hydroxyantipyrine and acetaminophen O-sulfate as biodistribution promoter. Biol Pharm Bull. 2001 Dec;24(12):1404-10.

物理化学性质

[ 密度 ]:
1.294g/cm3

[ 沸点 ]:
314.3ºC at 760mmHg

[ 熔点 ]:
184-186ºC(lit.)

[ 分子式 ]:
C₁₁H₁₂N₂O₂

[ 分子量 ]:
204.22500

[ 闪点 ]:
143.9ºC

[ 精确质量 ]:
204.09000

[ PSA ]:
47.16000

[ LogP ]:
1.19000

[ 蒸汽压 ]:
0.000199mmHg at 25°C

[ 折射率 ]:
1.63

[ 储存条件 ]:
2-8°C，密闭，干燥

MSDS

详细MSDS(安全技术说明书)

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: Irritant;

[ 风险声明 (欧洲) ]:
36/37/38

[ 安全声明 (欧洲) ]:
26-36

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

[ WGK德国 ]:
3

[ 海关编码 ]:
2933990090

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海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 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, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

文献

The effect of age and sex on metabolism and urinary excretion of antipyrine.

J. Gerontol. A. Biol. Sci. Med. Sci. 53(1) , M14-9, (1998)

Drug-metabolizing capacity is generally reduced in the elderly. The purpose of this investigation was to study antipyrine clearance and metabolite excretion in old subjects of both sexes.Saliva cleara...

The pharmacokinetics of antipyrine and three of its metabolites in the rabbit: intravenous administration of pure metabolites.

Pharm. Res. 8(12) , 1470-6, (1991)

Antipyrine (AP) is a commonly used probe of oxidative metabolism. Indirect evidence demonstrates formation rate limited disposition of its metabolites. Kinetic studies using antipyrine and its major m...

Separation and identification of the 4-hydroxyantipyrine sulphoconjugate.

J. Chromatogr. A. 576(1) , 103-9, (1992)

In a previous study we observed, during separation of total antipyrine metabolites by high-performance liquid chromatography and after enzymatic hydrolysis, an unidentified peak corresponding to an io...

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