39718-89-3

• 常用中文名：阿明洛芬
• 常用英文名：Alminoprofen
• CAS号：39718-89-3
• 分子式：C₁₃H₁₇NO₂
• 分子量：219.28000
• 相关类别： 原料药 解热镇痛药 非甾抗炎药
• 发布时间：2018-06-28 16:33:25
• 更新时间：2024-01-10 19:26:13
• Alminoprofen 是苯丙酸类非甾体抗炎药 (NSAID)。Alminoprofen 同时具有抑制分泌磷脂酶A2 (sPLA2) 活性和抗环氧化酶 (COX-2) 的活性。

名称

• 中文名: 阿明洛芬
• 英文名: alminoprofen
• 英文别名: tetraethyldipyrromethane; 1H-Pyrrole,2,2'-methylenebis[3,4-diethyl; 3,3',4,4'-Tetraethyl-2,2'-dipyrrolylmethane; rac Alminoprofen; 2-(p-methallylaminophenyl)-propionic acid; 2,2'-methylenebis(3,4-diethylpyrrole); (+/-)-2-{p-[(2-methylallyl)amino]phenyl}propionic acid

物化性质

• 密度: 1.107g/cm3
• 沸点: 373.1ºC at 760 mmHg
• 熔点: 107°
• 分子式: C₁₃H₁₇NO₂
• 分子量: 219.28000
• 闪点: 179.4ºC
• 精确质量: 219.12600
• PSA: 49.33000
• LogP: 2.93570
• 折射率: 1.571
• 储存条件: -20°C

生物活性

• 描述: Alminoprofen 是苯丙酸类非甾体抗炎药 (NSAID)。Alminoprofen 同时具有抑制分泌磷脂酶A2 (sPLA2) 活性和抗环氧化酶 (COX-2) 的活性。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> 磷脂
  研究领域 >> 炎症/免疫
  信号通路 >> 免疫及炎症 >> COX
• 靶点:

  sPLA2

  COX-2

• 体外研究: Alminoprofen通过抑制sPLA2和COX-2具有双重抗炎作用。Alminoprofen(从0到50μM) 对CRL-1517细胞系形成的PGE2水平诱导剂量相关的抑制反应[1]。
• 体内研究: 阿莫洛芬(100-300mg/kg；p、 o.)具有抗炎活性[1]。动物模型：Wistar大鼠组(足跖水肿)[1]剂量：100mg/kg给药：P.o.结果：在整个2小时观察期内,产生具有统计学意义的剂量依赖性拮抗作用。
• 参考文献:

  [1]. Raguenes-Nicol C, et al. Anti-inflammatory mechanism of alminoprofen: action on the phospholipid metabolism pathway. Biochem Pharmacol. 1999;57(4):433-443.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : UF5552000 CHEMICAL NAME : Propionic acid, 2-(4-(methallylamino)phenyl)- CAS REGISTRY NUMBER : 39718-89-3 LAST UPDATED : 199709 DATA ITEMS CITED : 11 MOLECULAR FORMULA : C13-H17-N-O2 MOLECULAR WEIGHT : 219.31 WISWESSER LINE NOTATION : QVY1&R DM1Y1&U1 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 550 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,79,1990 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 700 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,79,1990 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 660 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,79,1990 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 2400 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value 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: 14,207,1979 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 705 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,79,1990 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 980 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,79,1990 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - species unspecified DOSE/DURATION : 1780 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 9,165,1984 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 12740 mg/kg/52W-I TOXIC EFFECTS : Liver - changes in liver weight Kidney, Ureter, Bladder - changes in bladder weight Blood - normocytic anemia REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 14,2187,1986 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 10800 mg/kg/90D-I TOXIC EFFECTS : Gastrointestinal - ulceration or bleeding from stomach Blood - changes in leukocyte (WBC) count REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 14,3019,1986 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 910 mg/kg SEX/DURATION : female 17-21 day(s) after conception lactating female 21 day(s) post-birth TOXIC EFFECTS : Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - other neonatal measures or effects REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 14,3089,1986 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 2600 mg/kg SEX/DURATION : female 6-18 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Fertility - abortion REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 14,3079,1986