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非氨酯

非氨酯用途

Felbamate (FBM)是非镇静性抗痉挛剂,活性与NMDA受体相关。

非氨酯名称

[ CAS 号 ]:
25451-15-4

[ 中文名 ]:
非氨酯

[ 英文名 ]:
felbamate

[中文别名 ]:

[英文别名 ]:

Felbatol
3-propanediol dicarbamate
EINECS 247-001-4
Felbamatum
Felbamato
1,3-Propanediol,2-phenyl-,dicarbamate
1,3-bis-carbamoyloxy-2-phenyl-propane
1,3-Bis-carbamoyloxy-2-phenyl-propan
MFCD00865296
2-Phenyl-1,3-propanediyl dicarbamate

非氨酯生物活性

[ 描述 ]:

Felbamate (FBM)是非镇静性抗痉挛剂,活性与NMDA受体相关。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> iGluR

信号通路 >> 神经信号通路 >> iGluR

研究领域 >> 神经疾病

[参考文献]

[1]. Kuo CC, et al. Use-dependent inhibition of the N-methyl-D-aspartate currents by felbamate: a gating modifier with selective binding to the desensitized channels. Mol Pharmacol. 2004 Feb;65(2):370-80.

[2]. Harty TP, et al. Felbamate block of recombinant N-methyl-D-aspartate receptors: selectivity for the NR2B subunit. Epilepsy Res. 2000 Mar;39(1):47-55.

[相关活性小分子]

非氨酯物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
511.9±50.0 °C at 760 mmHg

[ 熔点 ]:
148-1500C

[ 分子式 ]:
C₁₁H₁₄N₂O₄

[ 分子量 ]:
238.240

[ 闪点 ]:
288.4±26.4 °C

[ 精确质量 ]:
238.095352

[ PSA ]:
104.64000

[ LogP ]:
1.20

[ 外观性状 ]:
白色结晶性粉末，熔点 151-152℃

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.559

[ 储存条件 ]:
Store at RT

[ 水溶解性 ]:
alcohol: soluble

非氨酯毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TZ1070000

CHEMICAL NAME :: 1,3-Propanediol, 2-phenyl-, dicarbamate

CAS REGISTRY NUMBER :: 25451-15-4

BEILSTEIN REFERENCE NO. :: 3345236

LAST UPDATED :: 199806

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C11-H14-N2-O4

MOLECULAR WEIGHT :: 238.27

WISWESSER LINE NOTATION :: ZVO1YR&1OVZ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 140 mg/kg

TOXIC EFFECTS :: Behavioral - sleep

REFERENCE :: PECAE5 Pediatric Emergency Care. (Williams & Wilkins, 428 E. Preston St., Baltimore, MD 21202) V.1- 1985- Volume(issue)/page/year: 11,369,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 1296 mg/kg/18D-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Gastrointestinal - other changes Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: PHPYDQ Pharmacotherapy (Carlisle, MA). (Pharmacotherapy Pub., Inc., 112 School St., Carlisle, MA 01741) V.1- 1981- Volume(issue)/page/year: 15,260,1995

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >5 gm/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: 11,931,1986

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >5 gm/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: 11,931,1986

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4 gm/kg

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

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 12,462,1969

非氨酯安全信息

[ 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 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

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

[ WGK德国 ]:
2

[ RTECS号 ]:
TZ1070000

[ 海关编码 ]:
2924299090

非氨酯合成路线

详细合成路线

非氨酯上下游产品

非氨酯上游产品

非氨酯下游产品

非氨酯制备

50g 2-苯基丙二酸二乙酯(I)在500ml无水乙醚中，用12g氢化铝锂还原。得到的23g2-苯基-1，3-丙二醇(II)和31gN，N-二甲基苯胺溶于100ml甲苯中，在-10℃下，将该混合液加到33g光气在150ml无水甲苯的溶液中。然后在-5-5℃维持反应20min，再用5%盐酸洗，用无水硫酸钠干燥。接着通人氨气至饱和，加热至回流，过滤得到非尔氨酯。

非氨酯海关

[ 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%

非氨酯文献

Pediatric super-refractory status epilepticus treated with allopregnanolone.

Ann. Neurol. 76(6) , 911-5, (2014)

Super-refractory status epilepticus is a life-threatening condition. Resistance to benzodiazepine and barbiturate treatment for this disorder is thought to be due to internalization of synaptic γ-amin...

Enhanced glutamatergic transmission reduces the anticonvulsant potential of lamotrigine but not of felbamate against tonic-clonic seizures.

Pharmacol. Rep. 59(4) , 462-6, (2007)

The efficacy of lamotrigine and felbamate against maximal electroshock (MES)-induced seizures was assessed under conditions mimicking the pharmacoresistance associated with an increased excitatory neu...

Behavioral and cognitive effects of anti-epileptic drugs.

Discov. Med. 9(45) , 138-44, (2010)

Anti-epileptic drugs (AEDs) have a variety of mechanisms of action which are reflected through different anticonvulsant activities and behavioral effects. Two categories of AEDs are considered based o...

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非氨酯