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托麦汀

托麦汀用途

Tolmetin 是一种具有口服活性的,有效的 COX 抑制剂,对人 COX-1 和 COX-2 的 IC50 值分别为 0.35 µM 和 0.82 µM。Tolmetin 属于非甾体类物质,具有强效的抗炎活性。

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托麦汀名称

[ CAS 号 ]:
26171-23-3

[ 中文名 ]:
托麦汀

[ 英文名 ]:
1-Methyl-5-p-toluoylpyrrole-2-acetic acid

[中文别名 ]:

托美汀

[英文别名 ]:

[3H]-Tolmetin
EINECS 247-497-2
Tolmetino
Tolmetine
Tolmetina
TOLMETIN
Tolmetinum
Tolectin
5-(p-toluoyl)-1-methylpyrrole-2-acetic acid
1-Methyl-5-p-toluoylpyrrole-2-acetic acid

托麦汀生物活性

[ 描述 ]:

Tolmetin 是一种具有口服活性的,有效的 COX 抑制剂,对人 COX-1 和 COX-2 的 IC50 值分别为 0.35 µM 和 0.82 µM。Tolmetin 属于非甾体类物质,具有强效的抗炎活性。

[ 相关类别 ]:

研究领域 >> 癌症

研究领域 >> 炎症/免疫

信号通路 >> 免疫及炎症 >> COX

[ 靶点 ]

Human COX-1:0.35 μM (IC50)

Human COX-2:0.82 μM (IC50)

[体外研究]

托美汀(0.25mm)对大鼠脑匀浆脂质过氧化无明显影响。托美汀(0.25,0.5,0.75,1mm)在大鼠脑匀浆中显示自由基清除特性,但不产生超氧阴离子[3]。托美汀(0.001-100μM)对HT-29结肠癌细胞具有一定的抗癌活性,且呈剂量依赖性[4]。托美汀(0-100μM)对成骨细胞生长无影响[5]。

[体内研究]

托美汀(30100mg/kg；灌胃；单次给药或每日两次,持续3天和14天)在单次给药后4h显示出最大的溃疡形成作用,而在体重180-200g的雄性Wistar大鼠中,重复给药3天和14天后,其溃疡作用显著降低。托美汀在100 mg/kg时引起胃损伤[2]。托美汀(5 mg/kg,每天两次,共5天)预处理可显著减轻喹啉酸(QA)诱导的神经毒性[3]。

[参考文献]

[1]. T D Warner, et al. Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: a full in vitro analysis. Proc Natl Acad Sci U S A. 1999 Jun 22;96(13):7563-8.

[2]. DADAŞ, Yakup, et al. Synthesis and anticancer activity of some novel tolmetin thiosemicarbazides. Marmara Pharmaceutical Journal 19(3) • April 2015

[3]. Etcheverry SB, et al. Three new vanadyl(IV) complexes with non-steroidal anti-inflammatory drugs (Ibuprofen, Naproxen and Tolmetin). Bioactivity on osteoblast-like cells in culture. J Inorg Biochem. 2002 Jan 1;88(1):94-100.

[4]. Etcheverry SB, et al. Three new vanadyl(IV) complexes with non-steroidal anti-inflammatory drugs (Ibuprofen, Naproxen and Tolmetin). Bioactivity on osteoblast-like cells in culture. J Inorg Biochem. 2002 Jan 1;88(1):94-100.

[5]. Etcheverry SB, et al. Three new vanadyl(IV) complexes with non-steroidal anti-inflammatory drugs (Ibuprofen, Naproxen and Tolmetin). Bioactivity on osteoblast-like cells in culture. J Inorg Biochem. 2002 Jan 1;88(1):94-100.

托麦汀物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
483.2±40.0 °C at 760 mmHg

[ 熔点 ]:
156ºC

[ 分子式 ]:
C₁₅H₁₅NO₃

[ 分子量 ]:
257.284

[ 闪点 ]:
246.0±27.3 °C

[ 精确质量 ]:
257.105194

[ PSA ]:
59.30000

[ LogP ]:
1.55

[ 外观性状 ]:
灰白色结晶粉末

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.582

[ 储存条件 ]:
存放于惰性气体之中;避免空气

[ 水溶解性 ]:
222 mg/L

托麦汀毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UX9287000

CHEMICAL NAME :: Pyrrole-2-acetic acid, 1-methyl-5-p-toluoyl-

CAS REGISTRY NUMBER :: 26171-23-3

BEILSTEIN REFERENCE NO. :: 0485305

LAST UPDATED :: 199612

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C15-H15-N-O3

MOLECULAR WEIGHT :: 257.31

WISWESSER LINE NOTATION :: T5NJ A1 BVR D1& E1VQ

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 :: 293 mg/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 25,1526,1975

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

ROUTE OF EXPOSURE :: Rectal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 744 mg/kg

TOXIC EFFECTS :: Biochemical - Metabolism (Intermediary) - effect on inflammation or mediation of inflammation

REFERENCE :: AFTOD7 Archivos de Farmacologia y Toxicologia. (Universidad Complutense, Facultad de Medicina, Departamento Coordinado de Farmacologia, Ciudad Universitaria, Madrid 3, Spain) V.1- 1975- Volume(issue)/page/year: 5,257,1979

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 914 mg/kg

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

REFERENCE :: FRPSAX Farmaco, Edizione Scientifica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 38,90,1983

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 600 mg/kg

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

REFERENCE :: FRPSAX Farmaco, Edizione Scientifica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 38,90,1983

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 680 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 8,45,1977

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

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1107 mg/kg

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

REFERENCE :: YHTPAD Yaoxue Tongbao. Bulletin of Pharmacology. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.13-23, 1978-88. For publisher information, see ZYZAEU. Volume(issue)/page/year: 19,460,1984

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - species unspecified

DOSE/DURATION :: 300 mg/kg

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

REFERENCE :: IJMRAQ Indian Journal of Medical Research. (Indian Council of Medical Research, Ansari Nagar, New Delhi 110 029, India) V.1- 1913- Volume(issue)/page/year: 81,621,1985 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 200 mg/kg/4D-I

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 52,454,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 1680 mg/kg/8W-I

TOXIC EFFECTS :: Brain and Coverings - other degenerative changes Liver - other changes Nutritional and Gross Metabolic - changes in metals, not otherwise specified

REFERENCE :: TOLED5 Toxicology Letters. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1977- Volume(issue)/page/year: (Suppl),245,1992 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 20600 ug/kg

SEX/DURATION :: female 21 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 30(1),25A,1984

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托麦汀安全信息

[ 危害码 (欧洲) ]:
Xi

[ 海关编码 ]:
2933990090

托麦汀合成路线

详细合成路线

托麦汀上下游产品

托麦汀上游产品

托麦汀下游产品

托麦汀海关

[ 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%

托麦汀