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去铁酮

去铁酮用途

Deferiprone是唯一口服有活性的铁螯合剂, 用于治疗地中海贫血中的输血性铁过载。

去铁酮名称

[ CAS 号 ]:
30652-11-0

[ 中文名 ]:
1,2-二甲基-3-羟基-4-吡啶酮

[ 英文名 ]:
Deferiprone

[中文别名 ]:

[英文别名 ]:

1,2-DIMETHYL-3-HYDROXYPYRID-4-ONE
3-hydroxy-1,2-dimethyl-pyrid-4-one
UNII-2BTY8KH53L
3-hydroxy-1,2-dimethylpyridin-4(1H)-one
Deferiprone
deferipnone
3-HYDROXY-1,2-DIMETHYL-4(1H)-PYRIDONE
Ferriprox
3-hydroxy-1,2-dimethyl-4-pyridinone
DMHP

去铁酮生物活性

[ 描述 ]:

Deferiprone是唯一口服有活性的铁螯合剂, 用于治疗地中海贫血中的输血性铁过载。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 心血管疾病

[参考文献]

[1]. Kontoghiorghes GJ, et al. Benefits and risks of deferiprone in iron overload in Thalassaemia and other conditions: comparison of epidemiological and therapeutic aspects with deferoxamine. Drug Saf. 2003;26(8):553-584.

[相关活性小分子]

去铁酮物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
232.7±40.0 °C at 760 mmHg

[ 熔点 ]:
272-275 °C(lit.)

[ 分子式 ]:
C₇H₉NO₂

[ 分子量 ]:
139.152

[ 闪点 ]:
94.5±27.3 °C

[ 精确质量 ]:
139.063324

[ PSA ]:
42.23000

[ LogP ]:
-0.22

[ 外观性状 ]:
白色针状

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.565

[ 储存条件 ]:
-20°C Freezer

[ 水溶解性 ]:
溶于热水

去铁酮MSDS

详细MSDS(安全技术说明书)

去铁酮毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UU7785940

CHEMICAL NAME :: 4(1H)-Pyridinone, 1,2-dimethyl-3-hydroxy-

CAS REGISTRY NUMBER :: 30652-11-0

BEILSTEIN REFERENCE NO. :: 1447108

LAST UPDATED :: 199803

DATA ITEMS CITED :: 11

MOLECULAR FORMULA :: C7-H9-N-O2

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 :: 2 gm/kg

TOXIC EFFECTS :: Cardiac - other changes

REFERENCE :: ATSUDG Archives of Toxicology, Supplement. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) No.1- 1978- Volume(issue)/page/year: 18,202,1996

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 600 mg/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: 13,413,1988

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 983 mg/kg

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

REFERENCE :: BLOOAW Blood. (Grune & Stratton, Inc., 465 S. Lincoln Dr., Troy, MO 63379) V.1- 1946- Volume(issue)/page/year: 76,2389,1990

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 1 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - food intake (animal) Gastrointestinal - ulceration or bleeding from stomach

REFERENCE :: BOMEEH BioMetals. (Rapid Communications of Oxford Ltd., The Old Malthouse, Paradise St., Oxford OX1 1LD, UK) V.5- 1992 Volume(issue)/page/year: 10,247,1997

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

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Mammal - species unspecified

DOSE/DURATION :: >1 gm/kg

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

REFERENCE :: ATSUDG Archives of Toxicology, Supplement. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) No.1- 1978- Volume(issue)/page/year: 18,202,1996 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 4200 mg/kg/4W-I

TOXIC EFFECTS :: Endocrine - changes in adrenal weight Endocrine - changes in spleen weight Endocrine - changes in thymus weight

REFERENCE :: MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 28(Suppl A),73,1992

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 52 gm/kg/52W-I

TOXIC EFFECTS :: Endocrine - changes in adrenal weight

REFERENCE :: MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 28(Suppl A),81,1992

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 8400 mg/kg/4W-I

TOXIC EFFECTS :: Endocrine - changes in adrenal weight Endocrine - changes in spleen weight Endocrine - changes in thymus weight

REFERENCE :: MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 28(Suppl A),73,1992

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 12 gm/kg/12W-I

TOXIC EFFECTS :: Blood - changes in other cell count (unspecified) Blood - changes in leukocyte (WBC) count Related to Chronic Data - death

REFERENCE :: BLOOAW Blood. (Grune & Stratton, Inc., 465 S. Lincoln Dr., Troy, MO 63379) V.1- 1946- Volume(issue)/page/year: 78,2727,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 3600 mg/kg/28D-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - somnolence (general depressed activity) Related to Chronic Data - death

REFERENCE :: BOMEEH BioMetals. (Rapid Communications of Oxford Ltd., The Old Malthouse, Paradise St., Oxford OX1 1LD, UK) V.5- 1992 Volume(issue)/page/year: 10,247,1997

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 10500 mg/kg/35W-I

TOXIC EFFECTS :: Cardiac - cardiomyopathy including infarction Liver - hepatitis (hepatocellular necrosis), diffuse Blood - changes in leukocyte (WBC) count

REFERENCE :: BOMEEH BioMetals. (Rapid Communications of Oxford Ltd., The Old Malthouse, Paradise St., Oxford OX1 1LD, UK) V.5- 1992 Volume(issue)/page/year: 10,247,1997

去铁酮安全信息

[ 危害码 (欧洲) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R22;R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36

[ WGK德国 ]:
3

[ RTECS号 ]:
UU7785940

[ 海关编码 ]:
2933399090

去铁酮合成路线

详细合成路线

去铁酮上下游产品

去铁酮上游产品

去铁酮下游产品

去铁酮制备

以 3-羟基-2-甲基-4 -吡啶酮为原料 ,经羟基保护、N-甲基化和脱保护基反应得到去铁剂去铁酮 ,总收率 4 9%。

去铁酮海关

[ 海关编码 ]: 2933399090

[ 中文概述 ]:
2933399090. 其他结构含非稠合吡啶环的化合物. 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, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

去铁酮