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托美丁钠(二水)

托美丁钠(二水)用途

Tolmetin sodium dihydrate 是一种非甾体抗炎剂,为非选择性的 COX 抑制剂。

托美丁钠(二水)名称

[ CAS 号 ]:
64490-92-2

[ 中文名 ]:
托美丁钠(二水)

[ 英文名 ]:
Tolmetin (sodium dihydrate)

[中文别名 ]:

[英文别名 ]:

EINECS 252-687-3
MFCD00079607
Tolmetin (sodium dihydrate)

托美丁钠(二水)生物活性

[ 描述 ]:

Tolmetin sodium dihydrate 是一种非甾体抗炎剂,为非选择性的 COX 抑制剂。

[ 相关类别 ]:

研究领域 >> 炎症/免疫

[ 靶点 ]

COX

[体外研究]

托美汀钠二水合物是非甾体抗炎剂。托美汀(0-100μM)对成骨细胞生长没有影响[2]。托美汀(0.25mM)剂量不会减弱大鼠脑匀浆中的脂质过氧化。托美汀(0.25,0.5,0.75,1mM)显示出自由基清除特性,但在大鼠脑匀浆中没有产生超氧阴离子[3]。

[体内研究]

托美汀(100mg/kg)引起胃损伤,并且在单剂量后4小时显示最大的溃疡形成作用,而在重复施用后3和14天后有效降低。托美汀产生明显的内皮损伤和炎症细胞浸润[1]。托美汀(5 mg/kg,腹腔注射,每天两次,连续5天)对大鼠的n NMDA受体结合没有影响[3]。

[动物实验]

大鼠[1]适应2周后，将大鼠随机分到不同组，并给予非选择性COX抑制剂，氨甲喋呤（AMG）（50和150 mg / kg）和托美汀（30和100 mg / kg）。作为选择性COX-2抑制剂，塞来昔布（CXIB; 20和60mg / kg）。在使用前立即将化合物悬浮在1％羧甲基纤维素（CMC）中，并通过管饲法以10mL / kg体积给药。控制组在同一卷中接收CMC。将每组的大鼠分成3个亚组，每组至少10只动物。亚组用单剂量（急性治疗组）或每日两次给药3天和14天（慢性治疗组）。为确保所有组在相同的时间内给药，接受少于14天NSAID的患者将获得CMC，直至他们开始指定的治疗。在最后一次给药后4小时，通过颈脱位处死大鼠。立即取出胃，沿较小的曲率打开并轻轻冲洗[1]。

[参考文献]

[1]. Morini G, et al. Morphological features of rat gastric mucosa after acute and chronic treatment with amtolmetin guacyl: comparison with non-selective and COX-2-selective NSAIDs. Digestion. 2003;68(2-3):124-32. Epub 2003 Nov 7.

[2]. 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.

[3]. Dairam A, et al. Non-steroidal anti-inflammatory agents, tolmetin and sulindac, attenuate oxidative stress in rat brain homogenate and reduce quinolinic acid-induced neurodegeneration in rat hippocampal neurons. Metab Brain Dis. 2006 Sep;21(2-3):221-33.

[相关活性小分子]

托美丁钠(二水)物理化学性质

[ 沸点 ]:
483.2ºC at 760 mmHg

[ 熔点 ]:
155-157 (dec.)

[ 分子式 ]:
C₁₅H₁₈NNaO₅

[ 分子量 ]:
315.30

[ 闪点 ]:
246ºC

[ PSA ]:
80.59000

[ LogP ]:
0.72830

[ 外观性状 ]:
结晶固体

[ 储存条件 ]:
-20°C Freezer

托美丁钠(二水)毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UX9280000

CHEMICAL NAME :: 1H-Pyrrole-2-acetic acid, 1-methyl-5-(4-methylbenzoyl)-, sodium salt, dihydrate

CAS REGISTRY NUMBER :: 64490-92-2

LAST UPDATED :: 199603

DATA ITEMS CITED :: 15

MOLECULAR FORMULA :: C15-H14-N-O3.Na.2H2-O

MOLECULAR WEIGHT :: 315.33

WISWESSER LINE NOTATION :: T5NJ A1 BVR D1& E1VO &-NA- &QH 2

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 :: 914 mg/kg

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

REFERENCE :: EPXXDW European Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #134763

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 612 mg/kg

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

REFERENCE :: EPXXDW European Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #134763

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1050 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Gastrointestinal - hypermotility, diarrhea

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 11,1099,1977

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >724 mg/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach Blood - changes in spleen

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 11,1099,1977

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 899 mg/kg

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

REFERENCE :: EPXXDW European Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #134763

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 550 mg/kg

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

REFERENCE :: EPXXDW European Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #134763

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 670 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Gastrointestinal - ulceration or bleeding from stomach

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 11,1099,1977

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >622 mg/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from large intestine Blood - changes in spleen

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 11,1099,1977 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 9360 mg/kg/26W-I

TOXIC EFFECTS :: Gastrointestinal - other changes Endocrine - adrenal cortex hyperplasia Blood - changes in cell count (unspecified)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 11,1117,1977

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3720 mg/kg/31D-I

TOXIC EFFECTS :: Endocrine - changes in spleen weight Blood - pigmented or nucleated red blood cells Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 11,1107,1977

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 43800 mg/kg/2Y-I

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach Blood - normocytic anemia

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 30,557,1979

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 33306 mg/kg/78W-I

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach Blood - normocytic anemia

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 30,557,1979

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 134 gm/kg/1Y-I

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach Blood - normocytic anemia

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 30,557,1979 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 163 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system

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: 8,158,1977

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1300 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion

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: 8,158,1977

托美丁钠(二水)安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H315

[ 警示性声明 ]:
P301 + P312 + P330

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R22;R38

[ 安全声明 (欧洲) ]:
S36

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

[ WGK德国 ]:
3

[ RTECS号 ]:
UX9280000