< 生产厂家价格 >

拉莫三嗪

拉莫三嗪用途

Lamotrigine(BW430C)可抑制5-HT和钠离子通道,可作用于惊厥。

点击显示

拉莫三嗪名称

[ CAS 号 ]:
84057-84-1

[ 中文名 ]:
那蒙特金

[ 英文名 ]:
lamotrigine

[中文别名 ]:

拉莫三嗪

[英文别名 ]:

Lamictal
Lamotrigin
6-(2,3-Dichlorophenyl)-1,2,4-triazine-3,5-diamine
EINECS 281-901-8
Crisomet
Lamictal CD
HYDROXYMETHYL PROGESTERONE
BW 430C
LAMOTRIGENE
LAMOTRIGINE API

拉莫三嗪生物活性

[ 描述 ]:

Lamotrigine(BW430C)可抑制5-HT和钠离子通道,可作用于惊厥。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

信号通路 >> 跨膜转运 >> 钠通道

研究领域 >> 神经疾病

[参考文献]

[1]. Goa, K.L., S.R. Ross, and P. Chrisp, Lamotrigine. A review of its pharmacological properties and clinical efficacy in epilepsy. Drugs, 1993. 46(1): p. 152-76.

[2]. Leach, M.J., C.M. Marden, and A.A. Miller, Pharmacological studies on lamotrigine, a novel potential antiepileptic drug: II. Neurochemical studies on the mechanism of action. Epilepsia, 1986. 27(5): p. 490-7.

[3]. Cheung, H., D. Kamp, and E. Harris, An in vitro investigation of the action of lamotrigine on neuronal voltage-activated sodium channels. Epilepsy Res, 1992. 13(2): p. 107-12.

[4]. Goldsmith, D.R., et al., Lamotrigine: a review of its use in bipolar disorder. Drugs, 2003. 63(19): p. 2029-50.

[相关活性小分子]

拉莫三嗪物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 沸点 ]:
503.1±60.0 °C at 760 mmHg

[ 熔点 ]:
177-181°C

[ 分子式 ]:
C₉H₇Cl₂N₅

[ 分子量 ]:
256.091

[ 闪点 ]:
258.1±32.9 °C

[ 精确质量 ]:
255.007858

[ PSA ]:
90.71000

[ LogP ]:
-0.19

[ 外观性状 ]:
白色结晶

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.706

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
DMSO: 20 mg/mL at 60 °C, soluble

拉莫三嗪MSDS

拉莫三嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XY5850700

CHEMICAL NAME :: 1,2,4-Triazine-3,5-diamine, 6-(2,3-dichlorophenyl)-

CAS REGISTRY NUMBER :: 84057-84-1

LAST UPDATED :: 199706

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C9-H7-Cl2-N5

MOLECULAR WEIGHT :: 256.11

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 19 mg/kg

TOXIC EFFECTS :: Behavioral - muscle contraction or spasticity Sense Organs and Special Senses (Eye) - effect, not otherwise specified Cardiac - EKG changes not diagnostic of specified effects

REFERENCE :: LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 342,1552,1993

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 2 mg/kg/30H-I

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)

REFERENCE :: PEDIAU Pediatrics. (American Academy of Pediatrics, P.O. Box 1034, Evanston, IL 60204) V.1- 1948- Volume(issue)/page/year: 98,294,1996

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 205 mg/kg

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

REFERENCE :: EPILAK Epilepsia (New York). (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) Ser.1-3: 1909-55; Ser.4: V.1- 1959- Volume(issue)/page/year: 25,655,1984

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 245 mg/kg

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

REFERENCE :: EPILAK Epilepsia (New York). (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) Ser.1-3: 1909-55; Ser.4: V.1- 1959- Volume(issue)/page/year: 25,655,1984

点击显示

拉莫三嗪安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
P301 + P310

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
R25

[ 安全声明 (欧洲) ]:
S45

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

[ WGK德国 ]:
3

[ RTECS号 ]:
XY5850700

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2933699090

拉莫三嗪合成路线

拉莫三嗪上下游产品

拉莫三嗪上游产品

拉莫三嗪下游产品

拉莫三嗪制备

2,3-二氯苯甲酸氯化为2,3-二氯苯甲酰氯,再和氰化亚铜反应后,和氨基胍缩合,最后在氢氧化钾作用下环合得拉莫三嗪.

1. 2,3-二氯苯甲酸的制备

在500ml耐酸高压釜中加入2,3-二氯甲苯15g(0.093mol)、98%硝酸60ml(1.38mol)和水300ml,搅拌升温至165~167ºC,釜内压力约0.5~6MPa下反应4h.冷却析晶,过滤,滤饼用5%NaOH水溶液250ml溶解,加活性炭1g,搅拌回流30min,趁热过滤,滤液加浓盐酸调至pH2 ,冷却析出白色晶体,结晶完全后过滤,得白色晶体2,3-二氯苯甲酸16.7g,收率94%,mp168.7~169.3ºC.(文献[10]报道mp167~169 ºC)

2. 2,3-二氯苯甲酰氯的制备

在反应瓶中加入上步产物2,3-二氯苯甲酸39.4g(0.2mol)和新蒸的氯化亚砜100ml(1.35mol),冷凝管上装置

充填无水CaCl2干燥管,搅拌加热至回流,搅拌回流反应21h.蒸除过量的氯化亚砜,再进行减压蒸馏.收集146~148 ºC/4.13kPa馏分,冷却固化后得白色固体2,3-二氯苯甲酰氯38.2g,收率91.2%,mp30.9~31.1ºC.

3. 2,3-二氯苯甲酰氰的制备

在反应瓶中加入氰化亚铜12g、碘化钾19.2g和无水二甲苯135ml,在氮气保护下,搅拌回流反应24h.用分水器除水.搅拌滴加上步产物2,3-二氯苯甲酰氯10g(0.48mol)的无水二甲苯36.6ml溶液,滴毕,搅拌回流反应72h. 冷却至室温,过滤,滤饼用无水二甲苯洗涤,滤液和洗液合并,减压蒸除溶剂,剩余物减压蒸馏,收集134~136 ºC/5.33kPa馏分.冷却固化后得白色固体2,3-二氯苯甲酰氰9.0g,收率93.8%,mp59.6~60.2 ºC.

4. 3,5-二氨基-6-(2,3-二氯苯基)-1,2,4-三嗪(拉莫三嗪)的合成

在反应瓶中加入氨基胍碳酸氢盐12g(0.088mol)慢慢加入8mol/L硝酸60ml,得到白色悬浮液,于25 ºC搅拌30min,再滴加上步产物2,3-二氯苯甲酰氰4.8g(0.024mol)的二甲基亚砜12ml溶液,滴毕,继续搅拌反应3h.室温静置7天.加0.88mol/L氨水调至pH12,于冰水浴冷却下继续搅拌反应30min.过滤,滤饼用水洗涤,减压干燥,加至10%KOH的甲醇溶液600ml中,搅拌加热至回流,搅拌回流反应12h.蒸除甲醇,剩余物中加入冰水120ml,搅拌30min,过滤,抽干,滤饼用异丙醇重结晶,得白色晶体3,5-二氨基-6-(2,3-二氯苯基)-1,2,4-三嗪(拉莫三嗪)0.9g,收率14.7%,mp215.8~218.2ºC.

点击显示

拉莫三嗪海关

[ 海关编码 ]: 2933699090

[ 中文概述 ]:
2933699090 其他结构上含非稠合三嗪环化合物. 增值税率:17.0% 退税率:9.0% 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 ]:
2933699090 other compounds containing an unfused triazine ring (whether or not hydrogenated) in the structure。Supervision conditions:None。VAT:17.0%。Tax rebate rate:9.0%。MFN tariff:6.5%。General tariff:20.0%

拉莫三嗪文献

Modeling nociception in zebrafish: a way forward for unbiased analgesic discovery.

PLoS ONE 10(1) , e0116766, (2015)

Acute and chronic pain conditions are often debilitating, inflicting severe physiological, emotional and economic costs and affect a large percentage of the global population. However, the development...

Development and validation of a GC/MS method for the simultaneous determination of levetiracetam and lamotrigine in whole blood.

J. Pharm. Biomed. Anal. 102 , 25-32, (2014)

A sensitive and accurate gas chromatography-mass spectrometric method was developed and validated for the simultaneous determination of levetiracetam and lamotrigine in whole blood. A solid-phase extr...

Functionalized nanocarrier combined seizure-specific vector with P-glycoprotein modulation property for antiepileptic drug delivery.

Biomaterials 74 , 64-76, (2015)

Despite optimal therapeutic regimen with currently available antiepileptic drugs (AEDs), approximately a third of epilepsy patients remain drug refractory. Region-specific overexpression of multidrug ...

更多文献

拉莫三嗪

拉莫三嗪用途

拉莫三嗪名称

拉莫三嗪生物活性

拉莫三嗪物理化学性质

拉莫三嗪MSDS

详细MSDS(安全技术说明书)

拉莫三嗪毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

拉莫三嗪安全信息

拉莫三嗪合成路线

详细合成路线

拉莫三嗪上下游产品

拉莫三嗪上游产品

拉莫三嗪下游产品

拉莫三嗪制备

拉莫三嗪海关

拉莫三嗪文献

相关药品：

推荐生产厂家/供应商：

相关化合物