4-(甲氨基)安替比林

4-(甲氨基)安替比林用途

4-Methylamino antipyrine 是一种 Metamizole 的活性代谢产物。Metamizole 是吡唑啉酮类非甾体抗炎药 (NSAID),可抑制 COX。Metamizole 是一种非阿片类镇痛药,可用于疼痛和发烧。4-Methylamino antipyrine 具有止痛,解热和相对较弱的抗炎特性。

4-(甲氨基)安替比林名称

[ CAS 号 ]:
519-98-2

[ 中文名 ]:
4-(甲氨基)安替比林

[ 英文名 ]:
4-Methylamino antipyrine

[中文别名 ]:

[英文别名 ]:

1-phenyl-2,3-dimethyl-4-methylamino-5-pyrazolone
4-(N-methyl)-aminoantipyrine
4-Methylamino Antipyrine
Noraminopyrine
Noramidopyrine
4-Monomethylaminoantipyrine
N-Methylaminophenazone
Monomethylaminoantipyrine
ANTIPYRINE,4-(METHYLAMINO)
4-methylaminophenazone

4-(甲氨基)安替比林生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 炎症/免疫

信号通路 >> 免疫及炎症 >> COX

[ 靶点 ]

COX[2][3]

[体外研究]

安替咪唑是一种前药,在室温和有氧的环境中,可以自发地、非酶地转化为4-甲基氨基安替比林。随后,4-甲基氨基安替比林的N-甲基侧链被氧化生成4-甲酰氨基安替比林,并进一步转化为4-氨基安替比林。水溶液和有氧条件下的安替比林由一组吡唑啉酮衍生物组成,其中4-甲基氨基安替比林在药理学上是最重要的[2]。

[体内研究]

本研究的目的是评估其活性代谢物4-甲基氨基安替比林在雄性仔猪肌肉注射一次甲咪唑后的药代动力学。8头健康雄性仔猪肌肉注射甲氨咪唑(100mg/kg)。4-甲基氨基安替比林血浆浓度在0.25~48h内可定量检测,平均最大浓度为47.59mg/mL,平均半衰期为8.57h。

[参考文献]

[1]. Burmańczuk A, et al. Pharmacokinetic investigations of the marker active metabolites 4-methylamino-antipyrine and 4-amino-antipyrine after intramuscular injection of metamizole in healthy piglets. J Vet Pharmacol Ther. 2016 Dec;39(6):616-620.

[2]. Campos C1, et al. Regulation of cyclooxygenase activity by metamizol. Eur J Pharmacol. 1999 Aug 13;378(3):339-47.

[3]. Ariza A, et al. Pyrazolones metabolites are relevant for identifying selective anaphylaxis to metamizole. Sci Rep. 2016 Mar 31;6:23845.

4-(甲氨基)安替比林物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
324.5±45.0 °C at 760 mmHg

[ 熔点 ]:
50-53ºC

[ 分子式 ]:
C₁₂H₁₅N₃O

[ 分子量 ]:
217.267

[ 闪点 ]:
150.0±28.7 °C

[ 精确质量 ]:
217.121506

[ PSA ]:
38.96000

[ LogP ]:
0.02

[ 蒸汽压 ]:
0.0±0.7 mmHg at 25°C

[ 折射率 ]:
1.619

[ 储存条件 ]:
-20℃

4-(甲氨基)安替比林MSDS

详细MSDS(安全技术说明书)

4-(甲氨基)安替比林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CD2995850

CHEMICAL NAME :: Antipyrine, 4-(methylamino)-

CAS REGISTRY NUMBER :: 519-98-2

BEILSTEIN REFERENCE NO. :: 0195234

LAST UPDATED :: 199612

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C12-H15-N3-O

MOLECULAR WEIGHT :: 217.30

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1288 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939- Volume(issue)/page/year: 30,599,1967

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 7 gm/kg

TOXIC EFFECTS :: Behavioral - analgesia

REFERENCE :: APFRAD Annales Pharmaceutiques Francaises. (SPPIF, B.P.22, F-41353 Vineuil, France) V.1- 1943- Volume(issue)/page/year: 35,489,1977

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1255 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NYKZAU Nippon Yakurigaku Zasshi. Japanese Journal of Pharmacology. (Nippon Yakuri Gakkai, c/o Kyoto Daigaku Igakubu Yakurigaku Kyoshitsu, Konoe-cho, Yoshida, Sakyo-ku, Kyoto 606, Japan) V.40- 1944- Volume(issue)/page/year: 71,609,1975

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Mammal - species unspecified

DOSE/DURATION :: 400 mg/kg

TOXIC EFFECTS :: Behavioral - analgesia

REFERENCE :: EJMCA5 European Journal of Medicinal Chemistry--Chimie Therapeutique. (Editions Scientifiques Elsevier, 29 rue Buffon, F-75005, Paris, France) V.9- 1974- Volume(issue)/page/year: 21,277,1986 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1691 mg/kg/3D-I

TOXIC EFFECTS :: Liver - changes in liver weight Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: JJPAAZ Japanese Journal of Pharmacology. (Japanese Pharmacological Soc., c/o Dept. of Pharmacology, Faculty of Medicine, Kyoto Univ., Sakyo-ku, Kyoto 606, Japan) V.1- 1951- Volume(issue)/page/year: 43,335,1987

4-(甲氨基)安替比林安全信息

[ 海关编码 ]:
2933199090

4-(甲氨基)安替比林合成路线

详细合成路线

4-(甲氨基)安替比林上下游产品

4-(甲氨基)安替比林上游产品

4-(甲氨基)安替比林下游产品

4-(甲氨基)安替比林海关

[ 海关编码 ]: 2933199090

[ 中文概述 ]:
2933199090. 其他结构上有非稠合吡唑环化合物. 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 ]:
2933199090. other compounds containing an unfused pyrazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%