盐酸瑞马酰胺

盐酸瑞马酰胺用途

Remacemide hydrochloride (FPL 12924AA) 是一种钠离子通道的中等强度抑制剂,是 N-methyl-D-aspartate (NMDA) 受体的弱无竞争力拮抗剂,对于 MK-801 结合的 IC50 值为 68 μM,对于 NMDA 电流的 IC50 值为 76 μM。Remacemide hydrochloride 是一种抗惊厥剂。

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盐酸瑞马酰胺名称

[ CAS 号 ]:
111686-79-4

[ 中文名 ]:
2-氨基-N-(1-甲基-1,2-二苯乙基)乙酰胺盐酸盐

[ 英文名 ]:
Remacemide hydrochloride

[英文别名 ]:

PR 934-423A
Remacemide HCl
Remacemide hydrochloride
REMACEMIDE HYDROCHLORIDE

盐酸瑞马酰胺生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> iGluR

信号通路 >> 跨膜转运 >> 钠通道

研究领域 >> 神经疾病

信号通路 >> 跨膜转运 >> iGluR

[ 靶点 ]

IC50: 68-76 μM (NMDA receptor)[1] IC50:160.6 μM(sodium channel)[2]

[体外研究]

Remacemide(盐酸盐)(0-1000μM) 以浓度依赖性方式阻断大鼠皮层突触体的电压门控Na+通道,IC50值为160.6μM[2]。

[体内研究]

低剂量和高剂量的Remacemide(100 mg/kg和150 mg/kg)治疗延迟了雌性Sprague-Dawley大鼠听觉/视觉辨别(AVD)任务表现的获得[3]。动物模型：雌性Sprague-Dawley大鼠(190-210g)[3]剂量：100mg/kg和150mg/kg给药：口胃灌胃；每天一次；7天的结果：增加了完成视听辨别(AVD)培训所需的课时。

[参考文献]

[1]. G C Palmer, et al. Neuroprotective properties of the uncompetitive NMDA receptor antagonist remacemide hydrochloride. Ann N Y Acad Sci. 1995 Sep 15;765:236-47; discussion 248.

[2]. Sarah Santangeli, et al. Na⁺ channel effects of remacemide and desglycinyl-remacemide in rat cortical synaptosomes. Eur J Pharmacol. 2002 Mar 1;438(1-2):63-8.

[3]. L K M Wright, et al. Behavioral effects associated with chronic ketamine or remacemide exposure in rats. Neurotoxicol Teratol. May-Jun 2007;29(3):348-59.

盐酸瑞马酰胺物理化学性质

[ 沸点 ]:
466.4ºC at 760mmHg

[ 分子式 ]:
C₁₇H₂₁ClN₂O

[ 分子量 ]:
304.81400

[ 闪点 ]:
235.9ºC

[ 精确质量 ]:
304.13400

[ PSA ]:
55.12000

[ LogP ]:
4.11260

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
7.09E-09mmHg at 25°C

[ 储存条件 ]:
室温

盐酸瑞马酰胺MSDS

详细MSDS(安全技术说明书)

盐酸瑞马酰胺毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AB4349500

CHEMICAL NAME :: Acetamide, 2-amino-N-(1-methyl-1,2-diphenylethyl)-, monohydrochloride, (+-)-

CAS REGISTRY NUMBER :: 111686-79-4

LAST UPDATED :: 199706

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C17-H20-N2-O.Cl-H

MOLECULAR WEIGHT :: 304.85

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 :: 897 mg/kg

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

REFERENCE :: TOXID9 Toxicologist. (Soc. of Toxicology, Inc., 475 Wolf Ledge Parkway, Akron, OH 44311) V.1- 1981- Volume(issue)/page/year: 8,84,1988

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 142 mg/kg

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

REFERENCE :: TOXID9 Toxicologist. (Soc. of Toxicology, Inc., 475 Wolf Ledge Parkway, Akron, OH 44311) V.1- 1981- Volume(issue)/page/year: 8,84,1988

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 781 mg/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from small intestine Gastrointestinal - necrotic changes

REFERENCE :: TOXID9 Toxicologist. (Soc. of Toxicology, Inc., 475 Wolf Ledge Parkway, Akron, OH 44311) V.1- 1981- Volume(issue)/page/year: 8,84,1988

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 51 mg/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from small intestine Gastrointestinal - necrotic changes

REFERENCE :: TOXID9 Toxicologist. (Soc. of Toxicology, Inc., 475 Wolf Ledge Parkway, Akron, OH 44311) V.1- 1981- Volume(issue)/page/year: 8,84,1988 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 12 gm/kg/30D-I

TOXIC EFFECTS :: Related to Chronic Data - death

REFERENCE :: TOXID9 Toxicologist. (Soc. of Toxicology, Inc., 475 Wolf Ledge Parkway, Akron, OH 44311) V.1- 1981- Volume(issue)/page/year: 8,84,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 5400 mg/kg/90D-I

TOXIC EFFECTS :: Related to Chronic Data - death

REFERENCE :: TOXID9 Toxicologist. (Soc. of Toxicology, Inc., 475 Wolf Ledge Parkway, Akron, OH 44311) V.1- 1981- Volume(issue)/page/year: 8,84,1988

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盐酸瑞马酰胺安全信息

[ 符号 ]:

GHS05, GHS07, GHS09

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H318-H400

[ 警示性声明 ]:
P273-P280-P305 + P351 + P338

[ 危害码 (欧洲) ]:
C

[ 危险品运输编码 ]:
UN 3077 9 / PGIII

[ RTECS号 ]:
AB4349500

[ 海关编码 ]:
2924299090

盐酸瑞马酰胺海关

[ 海关编码 ]: 2924299090

[ 中文概述 ]:
2924299090. 其他环酰胺（包括环氨基甲酸酯）（包括其衍生物以及他们的盐）. 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:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 包装

[ Summary ]:
2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

盐酸瑞马酰胺文献

The cognitive and psychomotor effects of remacemide and carbamazepine in newly diagnosed epilepsy.

Epilepsy Behav. 14(3) , 522-8, (2009)

An international trial comparing remacemide hydrochloride with carbamazepine was undertaken in individuals with newly diagnosed epilepsy using a novel double-blind, parallel-group, double triangular s...

Chronic exposure to NMDA receptor and sodium channel blockers during development in monkeys and rats: long-term effects on cognitive function.

Ann. N. Y. Acad. Sci. 993 , 116-22; discussion 123-4, (2003)

The effects of chronic administration of MK-801 (NMDA-receptor antagonist) and remacemide (sodium channel blocker) on monkey learning of several brain function tasks was assessed in juveniles (nine mo...

Coenzyme Q10 and remacemide hydrochloride ameliorate motor deficits in a Huntington's disease transgenic mouse model.

Neurosci. Lett. 315(3) , 149-53, (2001)

Huntington's disease (HD) is a progressive inherited neurodegenerative disorder, for which there is no effective therapy. The CARE-HD study, recently published, evaluated the ability of a combination ...

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