卡比多巴

卡比多巴用途

Carbidopa ((S)-(-)-Carbidopa) monohydrate 是一种外周型脱羧酶 (decarboxylase) 抑制剂,可用于帕金森病的研究。Carbidopa monohydrate 是一种选择性芳香烃受体 (AhR) 调节剂。Carbidopa monohydrate 抑制胰腺癌细胞和肿瘤生长。

卡比多巴名称

[ CAS 号 ]:
38821-49-7

[ 中文名 ]:
卡比多巴

[ 英文名 ]:
Carbidopa monohydrate

[中文别名 ]:

[英文别名 ]:

CARBIDOPA 1-HYDRATE,PHARMA
Carbidopa
(S)-Carbidopa
L-a-Methyldopahydrazine
CARBIDOPA MONOHYDRATE
(S)-(-)-CARBIDOPA MONOHYDRATE
a-Methyldopahydrazine
Lodosin
carbidopa [INN_en]
CARBIDOPA HYDRATE

卡比多巴生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 免疫及炎症 >> 芳基烃受体

研究领域 >> 神经疾病

[体外研究]

Carbidopa((S)-(-)-Carbidopa)一水合物表现出与BχPC3和Capan-2细胞中其他AhR配体相似的活性,即诱导CYP1A1和CYP1A2,它们被AhR拮抗剂如CH223191所抑制[1]。卡比多巴是一种芳香族-L-氨基酸脱羧酶抑制剂,对人肺类癌和小细胞肺癌细胞具有选择性的细胞毒性。卡比多巴是致命的(IC50=29μM)[3]。

[体内研究]

一水卡比多巴还可诱导AhR的核摄取,体内研究表明,1毫克/小鼠剂量的卡比多巴可显著抑制作为异种移植物的BχPC3细胞裸鼠的肿瘤生长[1]。

[参考文献]

[1]. Safe S. Carbidopa: a selective Ah receptor modulator (SAhRM). Biochem J. 2017;474(22):3763-3765. Published 2017 Nov 6.

[2]. Fermaglich J. Treatment of Parkinson's disease with carbidopa, a peripheral decarboxylase inhibitor, and levodopa. Med Ann Dist Columbia. 1974;43(12):587-591.

[3]. Gilbert JA, et al. 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):4365-4372.

卡比多巴物理化学性质

[ 密度 ]:
1.42 g/cm3

[ 沸点 ]:
528.7ºC at 760 mmHg

[ 分子式 ]:
C₁₀H₁₆N₂O₅

[ 分子量 ]:
244.244

[ 闪点 ]:
273.5ºC

[ 精确质量 ]:
244.105927

[ PSA ]:
125.04000

[ LogP ]:
0.97380

[ 储存条件 ]:
库房低温通风干燥

卡比多巴MSDS

详细MSDS(安全技术说明书)

卡比多巴毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MW5300000

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

CAS REGISTRY NUMBER :: 38821-49-7

LAST UPDATED :: 199707

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C10-H14-N2-O4.H2-O

MOLECULAR WEIGHT :: 244.28

WISWESSER LINE NOTATION :: ZMX1&VQ2R &QH

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 :: 4810 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Behavioral - ataxia

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 29,181,1974

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 352 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Behavioral - ataxia

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 29,181,1974

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3428 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - other changes Skin and Appendages - hair

REFERENCE :: SKKNAJ Sankyo Kenkyusho Nempo. Annual Report of Sankyo Research Laboratories. (Sankyo K.K. Sogo Kenkyusho, 1-2-58 Hiro-machi, Shinagawa-ku, Tokyo 140, Japan) No.15- 1963- Volume(issue)/page/year: 28,116,1976

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1750 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Behavioral - ataxia

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 29,181,1974

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 148 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Behavioral - ataxia

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 29,181,1974

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4955 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - ataxia Skin and Appendages - hair

REFERENCE :: SKKNAJ Sankyo Kenkyusho Nempo. Annual Report of Sankyo Research Laboratories. (Sankyo K.K. Sogo Kenkyusho, 1-2-58 Hiro-machi, Shinagawa-ku, Tokyo 140, Japan) No.15- 1963- Volume(issue)/page/year: 28,116,1976

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 519 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Behavioral - ataxia

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 29,181,1974

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >600 mg/kg

TOXIC EFFECTS :: Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory depression Kidney, Ureter, Bladder - hematuria

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 29,181,1974

卡比多巴安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H319

[ 警示性声明 ]:
P305 + P351 + P338

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

[ WGK德国 ]:
3

[ 海关编码 ]:
2932999099

卡比多巴海关

[ 海关编码 ]: 2928000090

[ 中文概述 ]:
2928000090 其他肼（联氨）及胲（羟胺）的有机衍生物。监管条件:无。增值税率:17.0%。退税率:9.0%。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 ]:
2928000090 other organic derivatives of hydrazine or of hydroxylamine VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:20.0%

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