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卡别多巴

卡别多巴用途

Carbidopa是多巴脱羧酶抑制剂,可作用于帕金森症。

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卡别多巴名称

[ CAS 号 ]:
28860-95-9

[ 中文名 ]:
卡比多巴

[ 英文名 ]:
Carbidopa

[中文别名 ]:

[英文别名 ]:

Carbidopa
(S)-Carbidopa
MFCD00069231
L-a-Methyldopahydrazine
a-Methyldopahydrazine
Lodosin
EINECS 249-271-9
carbidopa [INN_en]
(S)-(-)-Carbidopa
HMD

卡别多巴生物活性

[ 描述 ]:

Carbidopa是多巴脱羧酶抑制剂,可作用于帕金森症。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 神经疾病

[参考文献]

[1]. Durso, R., et al., Variable absorption of carbidopa affects both peripheral and central levodopa metabolism. J Clin Pharmacol, 2000. 40(8): p. 854-60.

[2]. Orlefors, H., et al., Carbidopa pretreatment improves image interpretation and visualisation of carcinoid tumours with 11C-5-hydroxytryptophan positron emission tomography. Eur J Nucl Med Mol Imaging, 2006. 33(1): p. 60-5.

[3]. Gilbert, J.A., L.M. Frederick, and M.M. Ames, The aromatic-L-amino acid decarboxylase inhibitor carbidopa is selectively cytotoxic to human pulmonary carcinoid and small cell lung carcinoma cells. Clin Cancer Res, 2000. 6(11): p. 4365-72.

[相关活性小分子]

卡别多巴物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
528.7±50.0 °C at 760 mmHg

[ 熔点 ]:
206 - 208ºC

[ 分子式 ]:
C₁₀H₁₄N₂O₄

[ 分子量 ]:
226.23

[ 闪点 ]:
273.5±30.1 °C

[ PSA ]:
115.81000

[ LogP ]:
-0.19

[ 外观性状 ]:
白色,结晶粉末

[ 蒸汽压 ]:
0.0±1.5 mmHg at 25°C

[ 折射率 ]:
1.641

[ 储存条件 ]:
库房低温通风干燥

卡别多巴MSDS

详细MSDS(安全技术说明书)

卡别多巴毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MW5298000

CHEMICAL NAME :: Hydrocinnamic acid, alpha-hydrazino-3,4-dihydroxy-alpha-methyl-, L-

CAS REGISTRY NUMBER :: 28860-95-9

LAST UPDATED :: 199504

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C10-H14-N2-O4

MOLECULAR WEIGHT :: 226.26

WISWESSER LINE NOTATION :: ZMX1&VQ1R CQ DQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2804 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 468 mg/kg

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 23400 mg/kg/90D-C

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes in urine composition Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2100 mg/kg

SEX/DURATION :: female 1-21 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - other developmental abnormalities

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2880 mg/kg

SEX/DURATION :: female 90 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina

MUTATION DATA

TYPE OF TEST :: Mutation in microorganisms

TEST SYSTEM :: Bacteria - Salmonella typhimurium

DOSE/DURATION :: 1 mg/plate

REFERENCE :: RCOCB8 Research Communications in Chemical Pathology and Pharmacology. (PJD Pub. Ltd., P.O. Box 966, Westbury, NY 11590) V.1- 1970- Volume(issue)/page/year: 49,415,1985 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4821 No. of Facilities: 17 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 303 (estimated) No. of Female Employees: 166 (estimated)

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卡别多巴安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

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

[ WGK德国 ]:
3

[ RTECS号 ]:
MW5298000

[ 海关编码 ]:
2932999099

卡别多巴制备

1、 Strecker法的合成路线。1.β-硝基-β-甲基-3-甲氧基-4-羟基苯乙烯（Ⅱ）的制备将香草醛、甲苯、硝基乙烷、冰醋酸和正丁胺反应得棕黄色结晶。2.α-（3-甲氧基-4-羟基苯基）丙酮（Ⅲ）及亚硫酸氢钠加成物的制备。将（Ⅱ）与甲苯一起加热加入铁粉和浓盐酸，回流反应结束后过滤，用EDTA水溶液洗涤甲苯溶液，无水硫酸钠干燥，过滤后加入亚硫酸氢钠水溶液，搅拌、析晶、过滤、晾干，得（Ⅳ）。3.α-肼基-α-甲基-β-（3-甲氧基-4-羟基苯基）丙腈（V）的制备将（N）、氰化钠、水及乙醚混合搅拌，加入水合肼，反应完毕后过滤，滤饼用水洗涤，经真空干燥得（V）。4.dl-α-肼基-α-甲基-β-（3,4-二羟基苯基）丙醇（Ⅵ）的制备将45%-48%氢溴酸冷至-8℃以下，通氯化氢至饱和。然后分批加入肼基腈，于-8℃搅拌反应8h。置冰箱中过夜。次日升温回收氯化氢，并于95℃反应3h，再将反应液减压蒸干，加入乙醇溶解残留物，冷至室温过滤，滤液用二乙胺中和至pH为6.4，再置冰箱中过夜，其后经处理得（Ⅵ）的粗品。用水精制得精品。5.将（Ⅵ）、L-卡比多巴晶种、浓盐酸加入沸水中溶解，加活性炭脱色过滤，滤液冷至60℃，在搅拌下再加一部分L-卡比多巴晶种。然后在1h内匀速降至35℃，保温搅拌0.5h，过滤，滤饼经干燥得L-卡比多巴。母液补加（Ⅵ），重复拆分操作。在升温至60℃时，可交叉加入D-卡比多巴晶种，以拆分右旋体。如此循环处理，一般可拆分6-7次左旋体，平均拆分收率37.3%（理论拆分收率50%）-

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卡别多巴海关

[ 海关编码 ]: 2932999099

[ 中文概述 ]:
2932999099. 其他仅含氧杂原子的杂环化合物. 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:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2932999099. other heterocyclic compounds with oxygen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

卡别多巴文献

A misguided 'pill in the pocket' approach with flecainide leading to cardiac arrest.

BMJ Case Rep. 2012 , doi:10.1136/bcr-2012-006868, (2012)

Beneficial effects of natural phenolics on levodopa methylation and oxidative neurodegeneration.

Brain Res. 1497 , 1-14, (2013)

Levodopa (L-DOPA) is widely used for symptomatic management in Parkinson's disease. We recently showed that (-)-epigallocatechin-3-gallate, a tea polyphenol, not only inhibits L-DOPA methylation, but ...

Three cases of impulse control disorder in Parkinson's disease patients receiving dopamine replacement therapy.

Ir. Med. J. 106(1) , 24-5, (2013)

Impulse control disorders (ICDs) are a known side effect of dopamine replacement therapy in patients with Parkinson's disease (PD). They can have devastating consequences for patients and their famili...

更多文献

卡别多巴

卡别多巴用途

卡别多巴名称

卡别多巴生物活性

卡别多巴物理化学性质

卡别多巴MSDS

详细MSDS(安全技术说明书)

卡别多巴毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

卡别多巴安全信息

卡别多巴制备

卡别多巴海关

卡别多巴文献

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