<生产厂家价格>

托卡朋

托卡朋用途

Tolcapone(Ro 40-7592)是口服活性的外周和中枢COMT抑制剂。

托卡朋名称

[ CAS 号 ]:
134308-13-7

[ 中文名 ]:
托卡朋

[ 英文名 ]:
Tolcapone

[中文别名 ]:

甲磺酸达氟沙星.甲达沙星.甲磺酸丹诺沙星

[英文别名 ]:

UNII-CIF6334OLY
tolcapone
tolcapone [INN_en]
3,4-Dihydroxy-4'-methyl-5-nitrobenzophenone
4'-methyl-3,4-dihydroxy-5-nitro-benzophenone
[14C]-Tolcapone
Tasmar (TN)
MFCD00866569
Tasmar
Ro 40-7592

托卡朋生物活性

[ 描述 ]:

Tolcapone(Ro 40-7592)是口服活性的外周和中枢COMT抑制剂。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> COMT

信号通路 >> 神经信号通路 >> COMT

研究领域 >> 神经疾病

[参考文献]

[1]. Neil E. Paterson, Jennifer Ricciardi, Caitlin Wetzler, et al. Sub-optimal performance in the 5-choice serial reaction time task in rats was sensitive to methylphenidate, atomoxetine and d-amphetamine, but unaffected by the COMT inhibitor tolcapone. Neuros

[2]. Saviana Di Giovanni, Simona Eleuteri, Katerina E. Paleologou, et al. Entacapone and Tolcapone, Two Catechol O-Methyltransferase Inhibitors, Block Fibril Formation of α-Synuclein and β-Amyloid and Protect against Amyloid-induced Toxicity. The Journal of Bi

[3]. Panos Bitsios, Panos Roussos1. Tolcapone, COMT polymorphisms and pharmacogenomic treatment of schizophrenia. Pharmacogenomics. 2001,12 (4): 559-566.

[4]. M.A. Vieira-Coelho, P. Soares-da-Silva. Ontogenic aspects of liver and kidney catechol-O- methyltransferase sensitivity to tolcapone. British Journal of Pharmacology.1996,117 (3):516-520.

[5]. J. Dingemanse, K. Jorga, G. Zurcher,et al. Pharmacokinetic-pharmacodynamic interaction between the COMT inhibitor tolcapone and single-dose levodopa. British Journal of Clinical Pharmacology 1995, 40 (3):253-262.

[相关活性小分子]

恩他卡朋 | 血清胺盐酸盐 | 奥匹卡朋 | 夫洛丙酮

托卡朋物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
485.6±45.0 °C at 760 mmHg

[ 熔点 ]:
126-128ºC

[ 分子式 ]:
C₁₄H₁₁NO₅

[ 分子量 ]:
273.241

[ 闪点 ]:
205.7±17.2 °C

[ 精确质量 ]:
273.063721

[ PSA ]:
103.35000

[ LogP ]:
4.07

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.661

[ 储存条件 ]:
-20°C Freezer

托卡朋毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: PC4952500

CHEMICAL NAME :: Methanone, (3,4-dihydroxy-5-nitrophenyl)(4-methylphenyl)-

CAS REGISTRY NUMBER :: 134308-13-7

LAST UPDATED :: 199709

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C14-H11-N-O5

MOLECULAR WEIGHT :: 273.26

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 :: >2 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory depression

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: 24(Suppl 10),S1513,199

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1600 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory depression

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: 24(Suppl 10),S1513,199 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 9300 mg/kg/4W-I

TOXIC EFFECTS :: Liver - changes in liver weight Related to Chronic Data - death

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: 24(Suppl 10),S1521,199

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 91 gm/kg/26W-C

TOXIC EFFECTS :: Nutritional and Gross Metabolic - weight loss or decreased weight gain

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: 24(Suppl 10),S1557,199

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 1120 mg/kg/4W-I

TOXIC EFFECTS :: Gastrointestinal - alteration in gastric secretion Kidney, Ureter, Bladder - other changes

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: 24(Suppl 10),S1537,199

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 25830 mg/kg/26W-I

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting

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: 24(Suppl 10),S1585,199

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 1760 mg/kg/15D-I

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting

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: 24(Suppl 10),S1513,199 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3 gm/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - other 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: 24(Suppl 10),S1631,199

托卡朋安全信息

[ 符号 ]:

GHS09

[ 信号词 ]:
Warning

[ 危害声明 ]:
H400

[ 警示性声明 ]:
P273

[ 危害码 (欧洲) ]:
N

[ 风险声明 (欧洲) ]:
50

[ 安全声明 (欧洲) ]:
61

[ 危险品运输编码 ]:
UN 3077 9 / PGIII

[ RTECS号 ]:
PC4952500

托卡朋合成路线

详细合成路线

托卡朋上下游产品

托卡朋上游产品

托卡朋下游产品

托卡朋文献

Real-time concurrent monitoring of apoptosis, cytosolic calcium, and mitochondria permeability transition for hypermulticolor high-content screening of drug-induced mitochondrial dysfunction-mediated hepatotoxicity.

Toxicol. Lett. 214(2) , 175-81, (2012)

A quantitative high-content screening (HCS) was suggested for the real-time monitoring of drug-induced mitochondrial dysfunction-mediated hepatotoxicity. This HCS is very advantageous in that it allow...

Telescoping phenomenon in pathological gambling: association with gender and comorbidities.

J. Nerv. Ment. Dis. 200(11) , 996-8, (2012)

The course of pathological gambling (PG) in women has been described as having a later age of initiation but a shorter time to problematic gambling ("telescoped"). This study examined evidence for tel...

Capture compound mass spectrometry sheds light on the molecular mechanisms of liver toxicity of two Parkinson drugs.

Toxicol. Sci. 113(1) , 243-53, (2010)

Capture compound mass spectrometry (CCMS) is a novel technology that helps understand the molecular mechanism of the mode of action of small molecules. The Capture Compounds are trifunctional probes: ...

更多文献

托卡朋