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巴氯芬

巴氯芬用途

Baclofen是GABA衍生物,可松弛骨骼肌肉。

巴氯芬名称

[ CAS 号 ]:
1134-47-0

[ 中文名 ]:
巴氯芬

[ 英文名 ]:
Baclofen

[中文别名 ]:

[英文别名 ]:

4-Amino-3-(4-chlorophenyl)butanoic acid
Lioresa
EINECS 214-486-9
(R,S)-Baclofen
b-(Aminomethyl)-4-chlorobenzenepropanoic Acid
baclon
b-(Aminomethyl)-p-chlorohydrocinnamic Acid
Benzenepropanoic acid, β-(aminomethyl)-4-chloro-
Z1YR DG&1VQ
Kemstro

巴氯芬生物活性

[ 描述 ]:

Baclofen是GABA衍生物,可松弛骨骼肌肉。

[ 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]. Bexis, S., et al., Baclofen prevents MDMA-induced rise in core body temperature in rats. Drug Alcohol Depend, 2004. 74(1): p. 89-96.

[2]. Perry, H.E., et al., Baclofen overdose: drug experimentation in a group of adolescents. Pediatrics, 1998. 101(6): p. 1045-8.

[相关活性小分子]

巴氯芬物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
364.3±32.0 °C at 760 mmHg

[ 熔点 ]:
208-210°C

[ 分子式 ]:
C₁₀H₁₂ClNO₂

[ 分子量 ]:
213.661

[ 闪点 ]:
174.1±25.1 °C

[ 精确质量 ]:
213.055649

[ PSA ]:
63.32000

[ LogP ]:
1.56

[ 外观性状 ]:
白色至非常淡的黄色固体

[ 蒸汽压 ]:
0.0±0.9 mmHg at 25°C

[ 折射率 ]:
1.577

[ 储存条件 ]:
通风低温干燥,与库房食品原料分开存放

[ 水溶解性 ]:
1 M HCl: 50 mg/mL

巴氯芬MSDS

巴氯芬毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MW5084200

CHEMICAL NAME :: Hydrocinnamic acid, beta-(aminomethyl)-p-chloro-

CAS REGISTRY NUMBER :: 1134-47-0

LAST UPDATED :: 199709

DATA ITEMS CITED :: 15

MOLECULAR FORMULA :: C10-H12-Cl-N-O2

MOLECULAR WEIGHT :: 213.68

WISWESSER LINE NOTATION :: Z1YR DG&1VQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 571 ug/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: APHRER Annals of Pharmacotherpy. (Harvey Whitney Books Co., POB 42696, Cincinnati, OH 45242) V. 26- 1992- Volume(issue)/page/year: 27,883,1993

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 3429 mg/kg

TOXIC EFFECTS :: Behavioral - coma Cardiac - pulse rate increase, without fall in BP Lungs, Thorax, or Respiration - respiratory obstruction

REFERENCE :: JTCTDW Journal of Toxicology, Clinical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.19- 1982- Volume(issue)/page/year: 32,291,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 18 mg/kg

TOXIC EFFECTS :: Behavioral - coma Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: JTCTDW Journal of Toxicology, Clinical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.19- 1982- Volume(issue)/page/year: 22,11,1984

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 14 mg/kg

TOXIC EFFECTS :: Behavioral - muscle weakness Behavioral - coma

REFERENCE :: JTCTDW Journal of Toxicology, Clinical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.19- 1982- Volume(issue)/page/year: 20,59,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 4286 ug/kg

TOXIC EFFECTS :: Behavioral - coma Cardiac - pulse rate Vascular - BP lowering not characterized in autonomic section

REFERENCE :: AJEMEN American Journal of Emergency Medicine. (WB Saunders, Philadelphia, PA) V.1- 1983- Volume(issue)/page/year: 4,552,1986

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 25 ug/kg/2D-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - coma

REFERENCE :: IJCPB5 International Journal of Clinical Pharmacology, Therapy and Toxicology. (Dustri-Verlag Dr. Karl Feistle, Postfach 49, D-8024 Munich-Deisenhofen, Fed. Rep. Ger.) V.6-10, 1972-74; V.18- 1980- Volume(issue)/page/year: 29,274,1991

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 145 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,576,1982

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 115 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 11,181,1980

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 78 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 11,181,1980

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 200 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,576,1982

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 103 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 11,181,1980

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 31 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: YAKUD5 Gekkan Yakuji. Pharmaceuticals Monthly. (Yakugyo Jihosha, Inaoka Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1959- Volume(issue)/page/year: 21,2069,1979 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1500 mg/kg/30D-I

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 31,871,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1820 mg/kg/26W-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - muscle weakness Behavioral - ataxia

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 31,871,1980 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5585 No. of Facilities: 35 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 497 (estimated) No. of Female Employees: 251 (estimated)

巴氯芬安全信息

[ 符号 ]:

GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H315-H317-H319-H334-H335-H360

[ 警示性声明 ]:
Missing Phrase - N15.00950417-P201-P261-P280-P284-P308 + P313

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T:Toxic;

[ 风险声明 (欧洲) ]:
R61;R25;R36/37/38;R42/43

[ 安全声明 (欧洲) ]:
53-22-36/37/39-45-52-36-26

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

[ WGK德国 ]:
3

[ RTECS号 ]:
MW5084200

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2922499990

巴氯芬合成路线

巴氯芬上下游产品

巴氯芬上游产品

巴氯芬下游产品

巴氯芬制备

将对氯苯甲醛与乙酰乙酸乙酯缩合生成对氯代苯亚甲基-双-乙酰乙酸乙酯。加热水水解得对氯代苯基戊二酸。用乙酐脱水环合生成对氯代苯基戊二酸酐。再用浓氨水胺化生成对氯代苯基戊二酸亚酰胺，最后开环、降解得对氯苯氨酪酸。其最后开环、降解的具体操作方法如下：将42.25gβ-（对氯苯基）戊二酸亚酰胺在搅拌下加入到含8.32g氢氧化钠的200ml水溶液中。混合物于50℃加热10min，冷却至10-15℃，滴加含40.9g氢氧化钠的200ml水溶液，20min后，加38.8g溴，在20-25℃搅拌8h，用浓盐酸仔细地将反应液的pH值调至7，随后即沉降出细的β-（对氯苯基）-γ-氨基-丁酸结晶，再由水中重结晶，熔点206-208℃。

巴氯芬海关

[ 海关编码 ]: 2922499990

[ 中文概述 ]:
2922499990 其他氨基酸及其酯及它们的盐（含有一种以上含氧基的除外）. 增值税率:17.0% 退税率:9.0% 监管条件:AB(入境货物通关单,出境货物通关单) 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, 乙醇胺及其盐应报明色度, 乙醇胺及其盐应报明包装

[ 监管条件 ]: A.入境货物通关单 B.出境货物通关单

[ 检验检疫 ]: P.进境动植物、动植物产品检疫 Q.出境动植物、动植物产品检疫 R.进口食品卫生监督检验 S.出口食品卫生监督检验 M.进口商品检验 N.出口商品检验

[ Summary ]:
HS:2922499990 other amino-acids, other than those containing more than one kind of oxygen function, and their esters; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:AB(certificate of inspection for goods inward,certificate of inspection for goods outward) MFN tariff:6.5% General tariff:30.0%

巴氯芬文献

GABA and its B-receptor are present at the node of Ranvier in a small population of sensory fibers, implicating a role in myelination.

J. Neurosci. Res. 93(2) , 285-95, (2014)

The γ-aminobutyric acid (GABA) type B receptor has been implicated in glial cell development in the peripheral nervous system (PNS), although the exact function of GABA signaling is not known. To inve...

Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.

Chem. Res. Toxicol. 23 , 171-83, (2010)

Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental...

Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).

J. Sci. Ind. Res. 65(10) , 808, (2006)

Drug-induced liver injury (DILI) is a significant concern in drug development due to the poor concordance between preclinical and clinical findings of liver toxicity. We hypothesized that the DILI typ...

更多文献

巴氯芬相关知识

巴氯芬说明书-作用-巴氯芬片副作用

2018-12-29 14:23:44

导读：巴氯芬为骨骼肌松弛药。机制尚不明，可能干扰兴奋性神经递质释放，抑制脊髓突触间的传导。它用于改善锥体束损害造成的肌张力增高的痉挛症状、不同原因造成的痉挛性偏瘫和截瘫，如多发性硬化、脑血管病、脊髓损伤和脊髓炎后遗症、儿童脑性瘫痪、破伤风、难治性呃逆；改善 Duchenne肌营养不良症患者中十二指...

巴氯芬