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苯磺保泰松

苯磺保泰松用途

Sulfinpyrazone (G-28315) 是可针对慢性和间歇性痛风性关节炎的一种口服有效的尿酸剂 (uricosuric agent)。Sulfinpyrazone 具有抗血栓和血小板抑制作用。

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苯磺保泰松名称

[ CAS 号 ]:
57-96-5

[ 中文名 ]:
(±)-磺吡酮

[ 英文名 ]:
(+/-)-Sulfinpyrazone

[中文别名 ]:

[英文别名 ]:

sulphinpyrazone
Diphenylpyrazone
Sulfinpyrazon
Anturane
Sulfoxyphenylpyrazolidine
EINECS 200-357-4
Enturan
Anturano
Enturen
ulfinpyrazone

苯磺保泰松生物活性

[ 描述 ]:

Sulfinpyrazone (G-28315) 是可针对慢性和间歇性痛风性关节炎的一种口服有效的尿酸剂 (uricosuric agent)。Sulfinpyrazone 具有抗血栓和血小板抑制作用。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 炎症/免疫

[体外研究]

亚磺吡唑酮(G-28315)刺激纤溶活性[2]。

[体内研究]

在高岭土致大鼠足肿胀模型中,亚磺吡唑酮(G-28315)口服30mg/kg可恢复明显延长的球蛋白溶解时间。除这些作用外,亚磺吡唑酮还可保护家兔在单次口服10-30mg/kg花生四烯酸诱导的猝死[2]。

[参考文献]

[1]. Margulies EH, White AM, Sherry S. Sulfinpyrazone: a review of its pharmacological properties and therapeutic use. Drugs. 1980;20(3):179‐197.

[2]. Rüegg M. Antithrombotic effects of sulfinpyrazone in animals: influence on fibrinolysis and sodium arachidonate-induced pulmonary embolism. Pharmacology. 1976;14(6):522‐536.

苯磺保泰松物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
590.8±42.0 °C at 760 mmHg

[ 熔点 ]:
>300 °C(lit.)

[ 分子式 ]:
C₂₃H₂₀N₂O₃S

[ 分子量 ]:
404.482

[ 闪点 ]:
311.1±27.9 °C

[ 精确质量 ]:
404.119476

[ PSA ]:
76.90000

[ LogP ]:
2.30

[ 外观性状 ]:
固体;White to Light yellow powder to crystal

[ 蒸汽压 ]:
0.0±1.7 mmHg at 25°C

[ 折射率 ]:
1.717

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
soluble

苯磺保泰松MSDS

苯磺保泰松毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UQ8575000

CHEMICAL NAME :: 3,5-Pyrazolidinedione, 1,2-diphenyl-4-(2-(phenylsulfinyl)ethyl)-

CAS REGISTRY NUMBER :: 57-96-5

BEILSTEIN REFERENCE NO. :: 0713597

LAST UPDATED :: 199612

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C23-H20-N2-O3-S

MOLECULAR WEIGHT :: 404.51

WISWESSER LINE NOTATION :: T5VNNV EHJ BR& CR& E2SO&R

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 29 mg/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 358 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 :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 154 mg/kg

TOXIC EFFECTS :: Brain and Coverings - recordings from specific areas of CNS Behavioral - excitement Lungs, Thorax, or Respiration - respiratory stimulation

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 298 mg/kg

TOXIC EFFECTS :: Brain and Coverings - recordings from specific areas of CNS Behavioral - excitement Lungs, Thorax, or Respiration - respiratory stimulation

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 100 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 :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 240 mg/kg

TOXIC EFFECTS :: Brain and Coverings - recordings from specific areas of CNS Behavioral - excitement Lungs, Thorax, or Respiration - respiratory stimulation

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 195 mg/kg

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

MUTATION DATA

TYPE OF TEST :: Sex chromosome loss and nondisjunction

TEST SYSTEM :: Mold - Aspergillus nidulans

DOSE/DURATION :: 1 gm/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 26,159,1974 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5494 No. of Facilities: 54 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 1923 (estimated) No. of Female Employees: 905 (estimated)

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苯磺保泰松安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
S36

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

[ WGK德国 ]:
3

[ RTECS号 ]:
UQ8575000

[ 海关编码 ]:
2933990090

苯磺保泰松合成路线

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苯磺保泰松上游产品

苯磺保泰松下游产品

苯磺保泰松海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮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, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

苯磺保泰松文献

Trophic activity of human P2X7 receptor isoforms A and B in osteosarcoma.

PLoS ONE 9(9) , e107224, (2014)

The P2X7 receptor (P2X7R) is attracting increasing attention for its involvement in cancer. Several recent studies have shown a crucial role of P2X7R in tumour cell growth, angiogenesis and invasivene...

MRP7/ABCC10 expression is a predictive biomarker for the resistance to paclitaxel in non-small cell lung cancer.

Mol. Cancer Ther. 7(5) , 1150-5, (2008)

We used the paclitaxel-resistant human small cell lung cancer subline PC-6/TAX1-1, selected from PC-6 cells by paclitaxel, to test whether MRP7/ABCC10 (ABCC10) confers paclitaxel resistance. We found ...

Ascorbate uptake in pig coronary artery endothelial cells.

Mol. Cell Biochem. 271(1-2) , 43-9, (2005)

Although smooth muscle and endothelial cells in pig coronary artery are morphologically and functionally distinct, ascorbate uptake has been characterized only in smooth muscle cells. Ascorbate transp...

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