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替宁酸

替宁酸用途

铁粉酸是一种尿酸利尿剂。噻吩酸具有一定的肝毒性[1][3]。

替宁酸名称

[ CAS 号 ]:
40180-04-9

[ 中文名 ]:
替宁酸

[ 英文名 ]:
Tienilic acid

[中文别名 ]:

[英文别名 ]:

Tienilic acid
Tienilico acido
Acidum tienilicum
TienilicAcid
Selacryn
Diflurex
[2,3-dichloro-4-(2-thenoyl)phenoxy]acetic acid
Acido tienilico
Acide tienilique
Ticrex

替宁酸生物活性

[ 描述 ]:

铁粉酸是一种尿酸利尿剂。噻吩酸具有一定的肝毒性[1][3]。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 代谢疾病

[体内研究]

Tienilic acid(大鼠和小鼠为100 mg/lg,猪和狗为5 mg/kg；PO和IV；单次剂量)仅存在于血浆中,通过胆汁和尿液禁食消除,在不同物种中表现出微小差异【2】。替尼酸(0-480 mg/kg；PO；持续28天)可降低血压、血清、尿酸血红蛋白,并增加S-GPT；诱导小群肝细胞的单细胞坏死[3]。动物模型：大鼠、小鼠、猪和狗【2】剂量：大鼠和小鼠100 mg/lg,猪和狗5 mg/kg给药：PO和IV；单次给药结果：仅在血液水平与血浆蛋白有重要结合的血浆中发现；药理作用数小时；在给药后的前48小时内,通过胆道,尤其是尿路禁食,几乎完全消除；在不同物种中测量的参数只有很小的差异。动物模型：雌性和雄性Sprague-Dawley大鼠【3】剂量：0、30、120和480 mg/kg给药：PO；28天结果：30 mg/kg时血压和血尿酸降低；在120和480 mg/kg时,血红蛋白略有下降,S-GPT升高；显著增加雄性大鼠的肝脏重量和血清镁浓度,而雌性大鼠的肝脏重量仅略有增加；此外,诱导小群肝细胞单细胞坏死。

[参考文献]

[1]. Lemieux G, et al, Baverel G. Metabolic effects in man of tienilic acid, a new diuretic with uricosuric properties. Nephron. 1978;20(1):54-64.

[2]. Levron, J.C., et al. Pharmacokinetic study of 2,3-dichloro 4- (2-thienyl keto14C) phenoxyacetic acid (tienilic acid) in animals. European Journal of Drug Metabolism and Pharmacokinetics 2, 107–120 (1977).

[3]. Oker-Blom C, et al. Toxicological studies on tienilic acid in rats. Toxicol Lett. 1980;6(2):93-99.

替宁酸物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
534.6±50.0 °C at 760 mmHg

[ 熔点 ]:
148-149ºC

[ 分子式 ]:
C₁₃H₈Cl₂O₄S

[ 分子量 ]:
331.17

[ 闪点 ]:
277.1±30.1 °C

[ 精确质量 ]:
329.952026

[ PSA ]:
91.84000

[ LogP ]:
3.07

[ 蒸汽压 ]:
0.0±1.5 mmHg at 25°C

[ 折射率 ]:
1.632

[ 储存条件 ]:
-20°C

替宁酸毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AG9300000

CHEMICAL NAME :: Acetic acid, (2,3-dichloro-4-(2-thienylcarbonyl)phenoxy)-

CAS REGISTRY NUMBER :: 40180-04-9

BEILSTEIN REFERENCE NO. :: 1260086

LAST UPDATED :: 199612

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C13-H8-Cl2-O4-S

MOLECULAR WEIGHT :: 331.17

WISWESSER LINE NOTATION :: T5SJ BVR BG CG DO1VQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 3571 ug/kg

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - urine volume decreased

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 6666 ug/kg

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 5 mg/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting Kidney, Ureter, Bladder - urine volume decreased

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1275 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 :: 318 mg/kg

TOXIC EFFECTS :: Kidney, Ureter, Bladder - urine volume increased

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 225 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 :: 3360 mg/kg/28D-I

TOXIC EFFECTS :: Vascular - BP lowering not characterized in autonomic section Liver - changes in liver weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 6300 mg/kg/14D-I

TOXIC EFFECTS :: Liver - other changes Kidney, Ureter, Bladder - other changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - hepatic microsomal mixed oxidase (dealkylation, hydroxylation, etc.)

MUTATION DATA

TYPE OF TEST :: Mutation in mammalian somatic cells

TEST SYSTEM :: Rodent - hamster Lung

DOSE/DURATION :: 100 umol/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 157,1,1985

替宁酸安全信息

[ 危害码 (欧洲) ]:
Xi

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

[ RTECS号 ]:
AG9300000

[ 海关编码 ]:
2934999090

替宁酸上下游产品

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替宁酸海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 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

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

替宁酸文献

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Drug resistance by Plasmodium falciparum remains a challenge in malaria chemotherapy. This paper will focus on physicochemical and drug metabolism characterization of a series of 4-aminoquinoline-3-hy...

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J. Biomol. Screen. 21 , 165-75, (2016)

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Chem. Res. Toxicol. 21(9) , 1814-22, (2008)

In vitro covalent binding assessments of drugs have been useful in providing retrospective insights into the association between drug metabolism and a resulting toxicological response. On the basis of...

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替宁酸