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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。

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)

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%）-

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...

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