苄噻嗪

苄噻嗪用途

Benzthiazide 是一种长效的利尿剂[1]和抗高血压剂。Benzthiazide 为碳酸酐酶 9 (carbonic anhydrase 9 (CA9)) 的抑制剂,对 CA9,CA2 和 CA1 的 Ki 值分别为 8.0,8.8 和 10 nM。Benzthiazide 能够抑制肿瘤细胞增殖[2]。

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苄噻嗪名称

[ CAS 号 ]:
91-33-8

[ 中文名 ]:
苄噻嗪

[ 英文名 ]:
Benzthiazide

[中文别名 ]:

苄硫噻嗪

[英文别名 ]:

Lemazide
benzotiazide
Exna
Benzothiazide
Benzthiazidum
EINECS 202-061-0
MFCD00078969
Freeuril
Aquatag
Dihydrex

苄噻嗪生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 碳酸酐酶

研究领域 >> 心血管疾病

[ 靶点 ]

Ki: 8.0 nM (CA9), 8.8 nM (CA2), 10 nM (CA1)[2]

[体外研究]

苯并噻嗪(0.4,2,10μM)以剂量依赖性方式在低氧条件下抑制癌细胞的增殖。苯并噻嗪是碳酸酐酶9(CA9)的抑制剂,CA9,CA2和CA1的Kis分别为8.0,8.8和10nM [2]。

[体内研究]

苯并噻嗪(1,1.5 mg/100 g BW)导致高催乳素血症大鼠尿钙排泄明显减少,钙和钠排泄分离[1]。

[参考文献]

[1]. Adler RA, et al. Hypercalciuria in hyperprolactinemic rats: effects of benzthiazide. Metabolism. 1986 Jul;35(7):668-72.

[2]. Lee HS, et al. Rational drug repositioning guided by an integrated pharmacological network of protein, disease and drug. BMC Syst Biol. 2012 Jul 2;6:80.

[相关活性小分子]

苄噻嗪物理化学性质

[ 密度 ]:
1.4176 (rough estimate)

[ 沸点 ]:
680.6 °C at 760 mmHg

[ 熔点 ]:
231-232° (U.S. patent); mp 238-239° (P'an)

[ 分子式 ]:
C₁₅H₁₄ClN₃O₄S₃

[ 分子量 ]:
431.93700

[ 闪点 ]:
365.4 °C

[ 精确质量 ]:
430.98300

[ PSA ]:
160.75000

[ LogP ]:
4.86900

[ 折射率 ]:
1.6100 (estimate)

[ 储存条件 ]:
室温

苄噻嗪MSDS

详细MSDS(安全技术说明书)

苄噻嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DK8400000

CHEMICAL NAME :: 2H-1,2,4-Benzothiadiazine-7-sulfonamide, 3-((benzylthio)menthyl)-6-chloro-, 1,1-dioxide

CAS REGISTRY NUMBER :: 91-33-8

LAST UPDATED :: 199610

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C15-H14-Cl-N3-O4-S3

MOLECULAR WEIGHT :: 431.95

WISWESSER LINE NOTATION :: T66 BSWM ENJ D1S1R& HG ISZW

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 :: >10 gm/kg

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

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 128,122,1960

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 422 mg/kg

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

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 128,122,1960

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >5 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,778,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 410 mg/kg

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

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 128,122,1960

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >5 gm/kg

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

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 128,122,1960

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 200 mg/kg

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

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 128,122,1960 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 84680 No. of Facilities: 68 (estimated) No. of Industries: 1 No. of Occupations: 6 No. of Employees: 2770 (estimated)

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苄噻嗪安全信息

[ 符号 ]:

GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H317-H334

[ 警示性声明 ]:
P261-P280-P342 + P311

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
42/43

[ 安全声明 (欧洲) ]:
26-36

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

[ WGK德国 ]:
2

[ RTECS号 ]:
DK8400000

[ 海关编码 ]:
2935009090

苄噻嗪海关

[ 海关编码 ]: 2935009090

[ 中文概述 ]:
2935009090 其他磺（酰）胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:35.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

苄噻嗪文献

Interactions of diuretics with a neutral temperature-responsive polymer: study by capillary electroporesis and dynamic light scattering.

J. Capill. Electrophor. Microchip Technol. 6(5-6) , 163-8, (1999)

Interactions between diuretics and a recently synthesized temperature-responsive neutral copolymer, poly(N-isopropyl acrylamide) (PNIPA) grafted with poly(ethyleneoxide) (PEO) (PNIPA-g-PEO) were inves...

Rational drug repositioning guided by an integrated pharmacological network of protein, disease and drug.

BMC Syst. Biol. 6 , 80, (2012)

The process of drug discovery and development is time-consuming and costly, and the probability of success is low. Therefore, there is rising interest in repositioning existing drugs for new medical i...

Rapid screening for diuretic doping agents in urine by C60-assisted laser-desorption-ionization-time-of-flight mass spectrometry.

J. Anal. Toxicol. 23(5) , 337-42, (1999)

This study describes a matrix-assisted laser-desorption-ionization (MALDI) mass spectrometry for rapid screening of 12 diuretics in spiked urine. C60 is used as the matrix for MALDI. Diuretics are dir...

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苄噻嗪