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奈非西坦

奈非西坦用途

Nefiracetam作用于Ro 5-4864引起的抽搐,是GABAergic,胆碱及单胺类的神经系统增强剂。

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奈非西坦名称

[ CAS 号 ]:
77191-36-7

[ 中文名 ]:
奈非西坦

[ 英文名 ]:
Nefiracetam

[中文别名 ]:

N-(2,6-二甲苯基)-2-氯乙酰胺

[英文别名 ]:

Nefiracetam
MFCD00209882
Dmmpa

奈非西坦生物活性

[ 描述 ]:

Nefiracetam作用于Ro 5-4864引起的抽搐,是GABAergic,胆碱及单胺类的神经系统增强剂。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> GABA受体

信号通路 >> 神经信号通路 >> GABA受体

研究领域 >> 神经疾病

[参考文献]

[1]. Nishizaki, T., et al., Nefiracetam modulates acetylcholine receptor currents via two different signal transduction pathways. Mol Pharmacol, 1998. 53(1): p. 1-5.

[2]. Shiotani, T., et al., Anticonvulsant actions of nefiracetam on epileptic EL mice and their relation to peripheral-type benzodiazepine receptors. Brain Res, 2000. 859(2): p. 255-61.

[3]. Sakurai, T., et al., Effects of N-(2,6-dimethylphenyl)-2-(2-oxo-1-pyrrolidinyl)acetamide (DM-9384) on learning and memory in rats. Jpn J Pharmacol, 1989. 50(1): p. 47-53.

[相关活性小分子]

奈非西坦物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
458.5±33.0 °C at 760 mmHg

[ 熔点 ]:
151-155°C

[ 分子式 ]:
C₁₄H₁₈N₂O₂

[ 分子量 ]:
246.305

[ 闪点 ]:
231.1±25.4 °C

[ 精确质量 ]:
246.136826

[ PSA ]:
49.41000

[ LogP ]:
1.53

[ 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 ]:
1.594

[ 储存条件 ]:
Store at RT

奈非西坦MSDS

奈非西坦毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UX9655650

CHEMICAL NAME :: 1-Pyrrolidineacetamide, N-(2,6-dimethylphenyl)-2-oxo-

CAS REGISTRY NUMBER :: 77191-36-7

LAST UPDATED :: 199801

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C14-H18-N2-O2

MOLECULAR WEIGHT :: 246.34

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 :: 1182 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 44,211,1994

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1940 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 44,211,1994

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >500 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 44,211,1994 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 10920 mg/kg/13W-I

TOXIC EFFECTS :: Liver - other changes Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Blood - other changes

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 44,214,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 109 gm/kg/2Y-I

TOXIC EFFECTS :: Liver - changes in liver weight Kidney, Ureter, Bladder - proteinuria Kidney, Ureter, Bladder - other changes in urine composition

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 44,220,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 16380 mg/kg/13W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - urine volume increased Kidney, Ureter, Bladder - other changes in urine composition

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 44,217,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 32760 mg/kg/2Y-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - other changes in urine composition Nutritional and Gross Metabolic - changes in sodium

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 44,228,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 8400 mg/kg/4W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - proteinuria Kidney, Ureter, Bladder - hematuria Kidney, Ureter, Bladder - inflammation, necrosis, or scarring of bladder

REFERENCE :: TOPADD Toxicologic Pathology. (c/o Dr. F.A. de la Iglesia, Warner-Lambert Co., Pharmaceutical Research Div., POB 1047, Ann Arbor, MI 48106) V.6(3/4)- 1978- Volume(issue)/page/year: 24,549,1996 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 11 gm/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 44,239,1994

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奈非西坦安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H319

[ 警示性声明 ]:
P305 + P351 + P338

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

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R22

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

[ RTECS号 ]:
UX9655650

[ 海关编码 ]:
2933790090

奈非西坦合成路线

奈非西坦上下游产品

奈非西坦上游产品

奈非西坦下游产品

奈非西坦制备

1-(羟基甲基)-2-吡咯啉酮(I)和2,6-二甲基苯胺(Ⅱ)缩合，得到奈非西坦，收率76%。

1. 2-氯-N-(2,6-二甲苯基)-乙酰胺的制备

在反应瓶中加入2,6-二甲基苯胺12.1g(0.1mol)和甲苯200ml,搅拌溶解后再加入Na2CO3 10.5g(0.1mol)的水(100ml)溶液,控制内温在20~35ºC搅拌滴加氯乙酰氯13.6g(0.12mol),滴毕,在同温度下搅拌2h.反应毕,冰浴冷却析晶,抽滤,干燥#得白色固体2-氯-N-(2,6-二甲苯基)-乙酰胺18.4g,收率93.2%,mp148~149 ºC.

2. 奈非西坦的合成

在反应瓶中加入甲苯270ml和甲醇钠10.8g(0.2mol),搅拌悬浮#再加入2-吡咯烷酮25.5g(0.3mol),缓慢加热至100~105ºC后搅拌3h.反应过程中大约蒸除甲醇和甲苯混合物16ml,冷至室温#加2-氯-N-(2,6-二甲苯基)-乙酰胺15.8g(0.08mol),在60~70ºC搅拌2h.向混合物中加水150ml,搅拌冷却,析晶后抽滤,干燥,滤饼用水200ml重结晶,得白色固体奈非西坦13.7g,收率69.5%,mp152~153ºC.

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奈非西坦海关

[ 海关编码 ]: 2933790090

[ 中文概述 ]:
2933790090 其他内酰胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:9.0% 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 ]:
2933790090. other lactams. VAT:17.0%. Tax rebate rate:9.0%. . MFN tariff:9.0%. General tariff:20.0%

奈非西坦文献

Investigation on urinary proteins and renal mRNA expression in canine renal papillary necrosis induced by nefiracetam.

Arch. Toxicol. 79(9) , 500-7, (2005)

The occurrence of renal papillary necrosis (RPN), seen only in dogs after repeated oral administration of nefiracetam, a neurotransmission enhancer, at a relatively high dose, is because of inhibition...

Nefiracetam and galantamine modulation of excitatory and inhibitory synaptic transmission via stimulation of neuronal nicotinic acetylcholine receptors in rat cortical neurons.

Neuroscience 160(2) , 484-91, (2009)

The cholinergic and glutamatergic systems are known to be downregulated in the brain of Alzheimer's disease patients. Galantamine and nefiracetam have been shown to potentiate the phasic activity of n...

Anticonvulsant properties of the novel nootropic agent nefiracetam in seizure models of mice and rats.

Epilepsia 46(6) , 811-8, (2005)

Nefiracetam (NEF) is a novel pyrrolidone-type nootropic agent, and it has been reported to possess various pharmacologic effects as well as cognition-enhancing effects. The present study focused on th...

更多文献

奈非西坦

奈非西坦用途

奈非西坦名称

奈非西坦生物活性

奈非西坦物理化学性质

奈非西坦MSDS

详细MSDS(安全技术说明书)

奈非西坦毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

奈非西坦安全信息

奈非西坦合成路线

详细合成路线

奈非西坦上下游产品

奈非西坦上游产品

奈非西坦下游产品

奈非西坦制备

奈非西坦海关

奈非西坦文献

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