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硝酸异山梨酯

硝酸异山梨酯用途

Isosorbide dinitrate (ISDN) 是一种 NO 供体,能防止心肌梗死 (MI) 引起的左室重构和心功能退化。

硝酸异山梨酯名称

[ CAS 号 ]:
87-33-2

[ 中文名 ]:
硝酸异山梨酯

[ 英文名 ]:
isosorbide dinitrate

[中文别名 ]:

[英文别名 ]:

Isorbid
Canranil
vasotrate
isosorbide dinitrate
1,4:3,6-Dianhydro-2,5-di-O-nitro-D-glucitol
D-Glucitol, 1,4:3,6-dianhydro-, dinitrate
Nitrol (VAN)
NITROL
MFCD00868238
EINECS 201-740-9

硝酸异山梨酯生物活性

[ 描述 ]:

Isosorbide dinitrate (ISDN) 是一种 NO 供体,能防止心肌梗死 (MI) 引起的左室重构和心功能退化。

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> 免疫及炎症 >> 一氧化氮合酶

[体内研究]

硝酸异山梨酯(3 mg/kg；气管内；13天)改善心肌梗死后心力衰竭大鼠模型的肺动脉压和心室重构[1]。硝酸异山梨酯后处理对大鼠心肌缺血再灌注损伤具有保护作用[2]。动物模型：5-6周龄雄性幼年Sprague-Dawley大鼠(200-250g)[1]剂量：3mg/kg给药：气管内给药；冠脉结扎后13天结果：心肌缩小,心肌梗死后左、右心室重构减轻。

[参考文献]

[1]. Wang X , et al. Intratracheal administration of isosorbide dinitrate improves pulmonary artery pressure and ventricular remodeling in a rat model of heart failure following myocardial infarction. Exp Ther Med. 2017 Aug;14(2):1399-1408.

[2]. Zhao X, et al. Cardioprotective Effect of Isosorbide Dinitrate Postconditioning Against Rat Myocardial Ischemia-Reperfusion Injury In Vivo. Med Sci Monit. 2019 Mar 2;25:1629-1636.

硝酸异山梨酯物理化学性质

[ 密度 ]:
1.7±0.1 g/cm3

[ 沸点 ]:
365.9±42.0 °C at 760 mmHg

[ 熔点 ]:
700C

[ 分子式 ]:
C₆H₈N₂O₈

[ 分子量 ]:
236.136

[ 闪点 ]:
186.6±29.9 °C

[ 精确质量 ]:
236.028061

[ PSA ]:
128.56000

[ LogP ]:
0.90

[ 外观性状 ]:
白色结晶粉末

[ 蒸汽压 ]:
0.0±0.8 mmHg at 25°C

[ 折射率 ]:
1.538

[ 储存条件 ]:
库房低温通风干燥,防火,与氧化剂分开存放

硝酸异山梨酯毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: LZ4385000

CAS REGISTRY NUMBER :: 87-33-2

LAST UPDATED :: 199703

DATA ITEMS CITED :: 19

MOLECULAR FORMULA :: C6-H8-N2-O8

MOLECULAR WEIGHT :: 236.16

WISWESSER LINE NOTATION :: T55 BO FOTJ DONW HONW

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: Standard Draize test

ROUTE OF EXPOSURE :: Administration onto the skin

SPECIES OBSERVED :: Rodent - rabbit

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 100 ug/kg

TOXIC EFFECTS :: Behavioral - coma Cardiac - pulse rate Cardiac - other changes

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 747 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 :: Administration onto the skin

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >3 gm/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 :: 670 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - respiratory depression

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1237 mg/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >40 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2 gm/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 :: 1050 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 :: 720 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 :: 1050 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 :: >40 mg/kg

TOXIC EFFECTS :: Behavioral - ataxia Skin and Appendages - hair

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1080 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 - rabbit

DOSE/DURATION :: >40 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia

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

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Mammal - species unspecified

DOSE/DURATION :: 1109 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 :: Intravenous

DOSE :: 260 mg/kg

SEX/DURATION :: female 6-22 day(s) after conception lactating female 20 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - sex ratio

MUTATION DATA

TYPE OF TEST :: Cytogenetic analysis

TEST SYSTEM :: Rodent - mouse Mammary gland

DOSE/DURATION :: 1 mmol/L/48H (Continuous)

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 5,141,1980 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3175 No. of Facilities: 171 (estimated) No. of Industries: 1 No. of Occupations: 3 No. of Employees: 2416 (estimated) No. of Female Employees: 1332 (estimated)

硝酸异山梨酯安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

[ 危害码 (欧洲) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R5;R22

[ 安全声明 (欧洲) ]:
S36

[ 危险品运输编码 ]:
UN 2907

[ 包装等级 ]:
II

[ 危险类别 ]:
1.1A

[ 海关编码 ]:
3004909090

硝酸异山梨酯合成路线

详细合成路线

硝酸异山梨酯上下游产品

硝酸异山梨酯上游产品

硝酸异山梨酯下游产品

硝酸异山梨酯制备

1.山梨醇溶液经脱水环合，与硝酸酯化而得。

2.制法：

于装有搅拌器、温度计的反应瓶中，加入发烟硝酸50g，浓硫酸7.5g，搅拌下冷却至10℃，慢慢滴加由脱水山梨醇（2）10g（固体）与1mL水微热溶解得到的液体，保持反应液温度在10～15℃，加完后保温反应2h。搅拌下将反应物倒入7倍量的冰水中，充分搅拌析晶。抽滤，水洗至中性，干燥，得粗品。将粗品加入1.5倍量的95%的乙醇中，加热溶解，活性炭脱色回流30min。趁热抽滤，冷至10℃以下，抽滤析出的结晶，乙醇洗涤，低温干燥，得硝酸异山梨醇酯（1），收率70%。

硝酸异山梨酯海关

[ 海关编码 ]: 2932999099

[ 中文概述 ]:
2932999099. 其他仅含氧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

[ Summary ]:
2932999099. other heterocyclic compounds with oxygen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

硝酸异山梨酯文献

In vitro and in vivo evaluation of novel osmotic pump tablets of isosorbide-5-mononitrate containing polyvinyl pyrrolidone (PVP) for controlled release.

Pharmazie 67(8) , 695-700, (2012)

A novel osmotic pump tablet with ethyl cellulose (EC) and polyvinyl pyrrolidone (PVP) as the semipermeable membrane and isosorbide-5-mononitrate (5-ISMN) as the model drug was formulated in this study...

Superoxide dismutases, SOD1 and SOD2, play a distinct role in the fat body during pupation in silkworm Bombyx mori.

PLoS ONE 10(2) , e0116007, (2015)

One way that aerobic biological systems counteract the generation of reactive oxygen species (ROS) is with superoxide dismutase proteins SOD1 and SOD2 that metabolize superoxide radicals to molecular ...

Early administration of isosorbide dinitrate improves survival of cyanide-poisoned rabbits.

Clin. Toxicol. (Phila.) 53(1) , 22-7, (2015)

More effective, rapidly delivered, safer antidotes are needed for cyanide poisoning. Previous study has demonstrated a beneficial effect of isosorbide dinitrate on the survival of cyanide-poisoned mic...

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