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托吡酯

托吡酯用途

Topiramate是镇痉化合物,能拮抗GluR5受体,还可作为GABA受体介导的电流阳性变构调节剂。

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托吡酯名称

[ CAS 号 ]:
97240-79-4

[ 中文名 ]:
托吡酯

[ 英文名 ]:
Topiramate

[中文别名 ]:

[英文别名 ]:

Topamax Sprinkle
Topiramate
Topimax
Tipiramato [Spanish]
Epitomax
McN-4853
topiramatum [Latin]
topiramatum
Tipiramate [French]
Tipiramate

托吡酯生物活性

[ 描述 ]:

Topiramate是镇痉化合物,能拮抗GluR5受体,还可作为GABA受体介导的电流阳性变构调节剂。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 谷氨酸受体

研究领域 >> 神经疾病

[参考文献]

[1]. Lyseng-Williamson KA, et al. Topiramate: a review of its use in the treatment of epilepsy. Drugs. 2007;67(15):2231-56.

[2]. Nakamura J, et al. Target pharmacology of topiramate, a new antiepileptic drug. Nihon Yakurigaku Zasshi. 2000 Jan;115(1):53-7.

[3]. Ormrod D, et al. Topiramate: a review of its use in childhood epilepsy. Paediatr Drugs. 2001;3(4):293-319.

[相关活性小分子]

托吡酯物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
438.7±55.0 °C at 760 mmHg

[ 熔点 ]:
125ºC

[ 分子式 ]:
C₁₂H₂₁NO₈S

[ 分子量 ]:
339.362

[ 闪点 ]:
219.1±31.5 °C

[ 精确质量 ]:
339.098785

[ PSA ]:
123.92000

[ LogP ]:
2.97

[ 外观性状 ]:
白色至灰白色结晶粉末

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.497

[ 储存条件 ]:
0-10°C;避免加热

[ 水溶解性 ]:
可溶于：甲醇

托吡酯MSDS

详细MSDS(安全技术说明书)

托吡酯毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: LS7083000

CAS REGISTRY NUMBER :: 97240-79-4

LAST UPDATED :: 199612

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C12-H21-N-O8-S

MOLECULAR WEIGHT :: 339.40

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 :: >1500 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: 14,342,1989

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托吡酯安全信息

[ 符号 ]:

GHS02, GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H225-H301 + H311 + H331-H370

[ 警示性声明 ]:
P210-P260-P280-P301 + P310-P311

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
26-36

[ 危险品运输编码 ]:
UN1230 - class 3 - PG 2 - Methanol, solution

[ WGK德国 ]:
3

[ RTECS号 ]:
LS7083000

托吡酯合成路线

详细合成路线

托吡酯上下游产品

托吡酯上游产品

托吡酯下游产品

托吡酯文献

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Kainic Acid-Induced Golgi Complex Fragmentation/Dispersal Shifts the Proteolysis of Reelin in Primary Rat Neuronal Cells: An In Vitro Model of Early Stage Epilepsy.

Mol. Neurobiol. , (2015)

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JAMA 311(18) , 1889-900, (2014)

Alcohol use disorders cause substantial morbidity and early mortality yet remain greatly undertreated. Medications are considerably underused.To conduct a systematic review and meta-analysis of the be...

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托吡酯