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氨苯蝶啶

氨苯蝶啶用途

Triamterene是压敏型上皮钠离子通道(ENaC)阻断剂,有利尿作用。

氨苯蝶啶名称

[ CAS 号 ]:
396-01-0

[ 中文名 ]:
氨苯蝶啶

[ 英文名 ]:
Triamterene

[中文别名 ]:

[英文别名 ]:

Triamterene
MFCD00006708
6-Phenylpteridine-2,4,7-triamine
EINECS 206-904-3

氨苯蝶啶生物活性

[ 描述 ]:

Triamterene是压敏型上皮钠离子通道(ENaC)阻断剂,有利尿作用。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钠通道

研究领域 >> 代谢疾病

[参考文献]

[1]. Busch, A.E., et al., Blockade of epithelial Na+ channels by triamterenes - underlying mechanisms and molecular basis. Pflugers Arch, 1996. 432(5): p. 760-6.

[2]. Gilfrich, H.J., et al., Pharmacokinetics of triamterene after i.v. administration to man: determination of bioavailability. Eur J Clin Pharmacol, 1983. 25(2): p. 237-41.

[相关活性小分子]

氨苯蝶啶物理化学性质

[ 密度 ]:
1.502 g/cm3

[ 沸点 ]:
573.4ºC at 760 mmHg

[ 熔点 ]:
316°C

[ 分子式 ]:
C₁₂H₁₁N₇

[ 分子量 ]:
253.26300

[ 闪点 ]:
11 °C

[ 精确质量 ]:
253.10800

[ PSA ]:
129.62000

[ LogP ]:
2.57700

[ 外观性状 ]:
黄色固体

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
<0.1 G/100 ML AT 20 ºC

氨苯蝶啶MSDS

详细MSDS(安全技术说明书)

氨苯蝶啶毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UO3470000

CHEMICAL NAME :: Pteridine, 2,4,7-triamino-6-phenyl-

CAS REGISTRY NUMBER :: 396-01-0

BEILSTEIN REFERENCE NO. :: 0266723

LAST UPDATED :: 199612

DATA ITEMS CITED :: 21

MOLECULAR FORMULA :: C12-H11-N7

MOLECULAR WEIGHT :: 253.30

WISWESSER LINE NOTATION :: T66 BN DN GN JNJ CZ EZ HR& IZ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 42 mg/kg/3W-I

TOXIC EFFECTS :: Liver - hepatitis (hepatocellular necrosis), zonal Nutritional and Gross Metabolic - body temperature increase

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 400 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 - rat

DOSE/DURATION :: 200 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 :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 285 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 :: 249 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 :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 620 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 :: 25077 ug/kg

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

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 25 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 :: 157 mg/kg/3W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2700 mg/m3/15D-C

TOXIC EFFECTS :: Endocrine - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 6370 mg/m3/13W-C

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 8190 mg/kg/13W-C

TOXIC EFFECTS :: Endocrine - other changes Blood - changes in leukocyte (WBC) count Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 21840 mg/kg/2Y-C

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Liver - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 34944 mg/kg/2Y-C

TOXIC EFFECTS :: Tumorigenic - neoplastic by RTECS criteria Liver - tumors

MUTATION DATA

TYPE OF TEST :: Sister chromatid exchange

TEST SYSTEM :: Rodent - hamster Lung

DOSE/DURATION :: 12600 ug/L

REFERENCE :: SNSHBT Senshokutai. Chromosome. (Sensyokutai Gakkai, Kaokusai Kirisutokyo Daigaku, Mitaka, Tokyo-to, Japan) No.1- 1946- Adopted new numbering in 1976. Volume(issue)/page/year: (20),574,1980 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5679 No. of Facilities: 60 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 587 (estimated) No. of Female Employees: 310 (estimated)

氨苯蝶啶安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H315-H319-H335

[ 警示性声明 ]:
P301 + P312 + P330-P305 + P351 + P338

[ 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;R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36/37/39-S45-S33-S24-S16-S7

[ 危险品运输编码 ]:
2811

[ WGK德国 ]:
3

[ RTECS号 ]:
UO3470000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2933990090

氨苯蝶啶制备

5-亚硝基-2，4，6-三氨基嘧啶和无水乙醇一起回流1h，加入部分量氰苄和乙醇钠，回流2h后再加入其余量氰苄和乙醇钠，继续回流5h，冷却至10℃左右，过滤，用沸水洗涤，得氨苯蝶啶粗品。将粗品、浓硫酸及活性炭加入水中，回流45min，趁热过滤，滤液加热至沸，加入ED-TA二钠盐，用浓氨水调节至pH9，过滤，洗涤，干燥，得成品。

氨苯蝶啶海关

[ 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%

氨苯蝶啶文献

[Clinical strategies for prevention of drug-induced urinary calculi].

Clin. Calcium 21(10) , 1457-63, (2011)

Drug-induced urinary calculi, although they account for only 1-2% of urinary calculi, deserve consideration because most of them are preventable. In the drug-containing calculi resulting from the crys...

Bioavailability study of triamterene and xipamide using urinary pharmacokinetic data following single oral dose of each drug or their combination.

J. Pharm. Biomed. Anal. 61 , 78-85, (2012)

An efficient chromatographic method for the simultaneous determination of triamterene (TRI) and xipamide (XIP) in urine samples, based on high performance liquid chromatography with photodiode array d...

Spectrophotometric and spectrodensitometric determination of triamterene and xipamide in pure form and in pharmaceutical formulation.

Drug Test. Anal. 2(3) , 113-21, (2010)

Sensitive and validated UV-spectrophotometric, chemometric and TLC-densitometric methods were developed for determination of triamterene (TRM) and xipamide (XIP) in their binary mixture, formulated fo...

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