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碘番酸

碘番酸用途

Iopanoic acid 是一个 5'-Deiodinase 抑制剂,也是一种碘造影剂。

碘番酸名称

[ CAS 号 ]:
96-83-3

[ 中文名 ]:
碘番酸

[ 英文名 ]:
Iopanoic acid

[中文别名 ]:

[英文别名 ]:

Choladine
iopanoic acid
Iopagnost
Polognost
MFCD00038687
EINECS 202-539-9
Iodopanoic acid
Telepaque
Cholevid
Jopanoic acid

碘番酸生物活性

[ 描述 ]:

Iopanoic acid 是一个 5'-Deiodinase 抑制剂,也是一种碘造影剂。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 内分泌

[ 靶点 ]

5'-Deiodinase[1]

[体外研究]

促甲状腺激素释放激素(TRH)诱导的促甲状腺激素(TSH)从垂体片段释放受到三碘甲基乙酸(10-7至10)的3,5,3'-三碘甲腺原氨酸(T3)(10-7M)的抑制-7 M),以及高浓度的碘化物(10-4或10-5 M)。在测试浓度下,碘酸没有显着影响[2]。

[体内研究]

在受孕后第18天和第19天给予怀孕大鼠的碘酸(IOP)不会改变产仔数(对照组：11.8±0.5胎儿达因,Iopanoic酸处理：11.6±0.6胎儿)或第20天体重(对照组：3.27±0.12) g,经碘酸处理：3.42±0.20g)。 Iopanoic acid治疗在肩胛间棕色脂肪组织(IBAT)和脑中产生显着的5'-脱碘酶(5'D)活性阻断;相反,肝5'D未被修饰。在第20天,与对照胎儿相比,在IBAT中3,5,3'-三碘甲状腺素(T3)含量相似,并且在Iopanoic酸处理的胎儿的脑和肝核中略微增加(p <0.05)。然而,当给予成年大鼠时,Iopanoic acid使IBAT核T3含量和血浆T3浓度显着降低。在足月时,碘酸对胎儿IBAT 5'D活性的抑制与第20天一样有效[1]。

[细胞实验]

大鼠脑垂体碎片由Medium-199灌注。在90分钟的平衡期后，灌注持续135分钟，有或没有包含在3,5,3'-三碘甲腺原氨酸（T3）10-7M，三碘甲基乙酸（TRIAC）（储备溶液10-4）的超融合培养基中。 M在20％甲醇中，终浓度10-8至10-6M），碘酸（原液10-3M在0.2M NaOH中，最终浓度10-7至10-5M）或碘化钾10-7在灌注之后是6分钟的促甲状腺激素释放激素（TRH）脉冲[2]。

[动物实验]

使用最初重180至200g的Wistar大鼠。在妊娠第18天开始给予Iopanoic acid（IOP）。怀孕大鼠每12小时皮下注射10mg碘酸，从妊娠第18天到第12天，在妊娠第20天或第22天早晨被杀死。对照动物接受具有相同时间的载体溶液。通过给予成年雄性大鼠（220-250g体重）的碘帕酸（IOP）以相同的剂量和剂量来评估降低肩胛上棕色脂肪组织（IBAT）核3,5,3'-三碘甲状腺素（T3）的碘酸效力。两天内在怀孕水坝中的时间表。剖腹产在18只（仅未治疗的动物），妊娠20和22天进行。通过斩首杀死胎儿，并去除IBAT，脑和肝脏。组织样品立即在液氮中冷冻，但来自几个22日龄胎儿的棕色脂肪除外，其直接在0.25M蔗糖中匀浆以进行线粒体分离[1]。

[参考文献]

[1]. Tuca A, et al. Inhibition of iodothyronine 5'-deiodinase by iopanoic acid does not block nuclear T3 accumulation during rat fetal development. Pediatr Res. 1994 Jan;35(1):91-5.

[2]. Szabolcs I, et al. Effects of triiodothyronine, triiodothyroacetic acid, iopanoic acid and iodide on the thyrotropin-releasing hormone-induced thyrotropin release from superfused rat pituitary fragments. Acta Endocrinol (Copenh). 1991 Oct;125(4):427-34.

[相关活性小分子]

碘番酸物理化学性质

[ 密度 ]:
2.426g/cm3

[ 沸点 ]:
529.1ºC at 760mmHg

[ 熔点 ]:
153 °C

[ 分子式 ]:
C₁₁H₁₂I₃NO₂

[ 分子量 ]:
570.93200

[ 闪点 ]:
273.8ºC

[ 精确质量 ]:
570.80000

[ PSA ]:
63.32000

[ LogP ]:
4.31710

[ 外观性状 ]:
白色 -微浅黄红色晶体 -粉末

[ 折射率 ]:
1.732

[ 储存条件 ]:
2-8°C

碘番酸MSDS

详细MSDS(安全技术说明书)

碘番酸毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MW5075000

CHEMICAL NAME :: Hydrocinnamic acid, 3-amino-alpha-ethyl-2,4,6-triiodo-

CAS REGISTRY NUMBER :: 96-83-3

BEILSTEIN REFERENCE NO. :: 2220381

LAST UPDATED :: 199710

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C11-H12-I3-N-O2

MOLECULAR WEIGHT :: 570.94

WISWESSER LINE NOTATION :: ZR BI DI FI C1Y2&VQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 86 mg/kg/1W-I

TOXIC EFFECTS :: Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: ARDEAC Archives of Dermatology. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.82- 1960- Volume(issue)/page/year: 123,387,1987

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 60 mg/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting Blood - thrombocytopenia Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: CTOXAO Clinical Toxicology. (New York, NY) V.1-18, 1968-81. For publisher information, see JTCTDW. Volume(issue)/page/year: 18,221,1981

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1540 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 14,232,1969

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1520 mg/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: -,103,1990

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 280 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 14,232,1969

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 6600 mg/kg

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

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 13,997,1970

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1230 mg/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: -,103,1990

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 320 mg/kg

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

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 13,997,1970 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2200 mg/kg

SEX/DURATION :: female 1-22 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

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: 7,425,1984

碘番酸安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

[ 风险声明 (欧洲) ]:
20/21/22

[ 安全声明 (欧洲) ]:
S22-S26-S36/37/39

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

[ RTECS号 ]:
NW5075000

[ 海关编码 ]:
2922499990

碘番酸合成路线

详细合成路线

碘番酸上下游产品

碘番酸上游产品

碘番酸下游产品

碘番酸制备

由间硝基苯甲醛（见C7H5NO3，[99-61-6]）经缩合、还原、酸化、碘化而得。1.缩合将正丁酸酐及干燥的正丁酸钠加入干燥的反应锅内，搅拌加热去水分。加入间硝基苯甲醛，在135-140℃下反应7h左右。冷却，放入冰水中析出黑褐色沉淀。甩滤，洗净焦性油，得缩合物粗品。将其溶于稀氨水中，在搅拌下加活性炭的白陶土加热脱色，过滤后滤液用稀硫酸化结晶。甩滤，用水洗涤滤饼，干燥，得间硝基-α-乙基肉桂酸（C11H11NO4），为淡黄色结晶，熔点141-143℃，收率70%以上。2.收还、酸化将间硝基-α-乙基肉桂酸溶于氢氧化钠溶液中，加热至75℃，在搅拌下逐步加入铝镍合金和铝粉，控制温度在80-84℃，加料完毕，继续保温反应0.5h。至达终点后，过滤。滤液用盐酸酸化，析出沉啶，过滤，滤饼即间氨基-α-乙基苯丙酸盐酸盐（C11H15NO2·HCL）。3.碘化在间氨基-α-乙基苯丙酸的水溶液中加二氯乙烷，在搅拌下加入一氯化碘酸溶液反应。得到的粗品用二氯乙烷精制，即得碘番酸。

碘番酸海关

[ 海关编码 ]: 2922499990

[ 中文概述 ]:
2922499990 其他氨基酸及其酯及它们的盐（含有一种以上含氧基的除外）. 增值税率:17.0% 退税率:9.0% 监管条件:AB(入境货物通关单,出境货物通关单) 最惠国关税:6.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乙醇胺及其盐应报明色度, 乙醇胺及其盐应报明包装

[ 监管条件 ]: A.入境货物通关单 B.出境货物通关单

[ 检验检疫 ]: P.进境动植物、动植物产品检疫 Q.出境动植物、动植物产品检疫 R.进口食品卫生监督检验 S.出口食品卫生监督检验 M.进口商品检验 N.出口商品检验

[ Summary ]:
HS:2922499990 other amino-acids, other than those containing more than one kind of oxygen function, and their esters; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:AB(certificate of inspection for goods inward,certificate of inspection for goods outward) MFN tariff:6.5% General tariff:30.0%

碘番酸文献

Regulation and function of deiodinases during decidualization in female mice.

Endocrinology 155(7) , 2704-17, (2014)

Thyroid dysfunction during human pregnancy is closely related to serious pregnancy outcome. However, the regulation and function of thyroid hormones during early pregnancy are largely unknown. We foun...

Crystallographic analysis reveals the structural basis of the high-affinity binding of iophenoxic acid to human serum albumin.

BMC Struct. Biol. 11 , 18, (2011)

Iophenoxic acid is an iodinated radiocontrast agent that was withdrawn from clinical use because of its exceptionally long half-life in the body, which was due in part to its high-affinity binding to ...

Liquid chromatography-electrospray ionization mass spectrometry for direct identification and quantification of iophenoxic acid in serum.

J. Chromatogr. B. Analyt. Technol. Biomed. Life Sci. 832(1) , 144-57, (2006)

A liquid chromatographic-electrospray ionization mass spectrometric technique was developed for direct quantitation of iophenoxic acid (IA) in serum. IA was spiked into canine, feline, bovine, equine,...

更多文献

碘番酸