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尼可地尔

尼可地尔用途

【用途1】
用于冠心病、心绞痛的预防
【用途2】
抗心绞痛药。有选择性扩张冠状动脉，持续增加冠脉流量，抑制冠脉痉挛的作用。用于各种心绞痛。

尼可地尔名称

[ CAS 号 ]:
65141-46-0

[ 中文名 ]:
尼可地尔

[ 英文名 ]:
Nicorandil

[中文别名 ]:

[英文别名 ]:

3-Pyridinecarboxamide, N-[2-(nitrooxy)ethyl]-
Nitorubin
Perisalol
2-(pyridine-3-carbonylamino)ethyl nitrate
2-[(Pyridin-3-ylcarbonyl)amino]ethylnitrat
Nicorandil
Ikorel
SG-75
Dancor
EINECS 265-514-1

尼可地尔生物活性

[ 描述 ]:

Nicorandil 钾离子通道活化剂。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钾通道

研究领域 >> 心血管疾病

[参考文献]

[1]. Nakae, I., et al., Effects of intravenous nicorandil on coronary circulation in humans: plasma concentration and action mechanism. J Cardiovasc Pharmacol, 2000. 35(6): p. 919-25.

[2]. Sauzeau, V., et al., Cyclic GMP-dependent protein kinase signaling pathway inhibits RhoA-induced Ca2+ sensitization of contraction in vascular smooth muscle. J Biol Chem, 2000. 275(28): p. 21722-9.

[相关活性小分子]

尼可地尔物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
456.7±25.0 °C at 760 mmHg

[ 熔点 ]:
92ºC

[ 分子式 ]:
C₈H₉N₃O₄

[ 分子量 ]:
211.175

[ 闪点 ]:
230.0±23.2 °C

[ 精确质量 ]:
211.059311

[ PSA ]:
97.04000

[ LogP ]:
0.72

[ 外观性状 ]:
白色或灰白色粉末

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.548

[ 储存条件 ]:
2-8°C

尼可地尔MSDS

详细MSDS(安全技术说明书)

尼可地尔毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: US4667600

CHEMICAL NAME :: 3-Pyridinecarboxamide, N-(2-(nitrooxy)ethyl)-

CAS REGISTRY NUMBER :: 65141-46-0

LAST UPDATED :: 199612

DATA ITEMS CITED :: 15

MOLECULAR FORMULA :: C8-H9-N3-O4

MOLECULAR WEIGHT :: 211.20

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 :: 1220 mg/kg

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

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 35,1627,1984

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1100 mg/kg

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

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 35,1627,1984

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1200 mg/kg

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

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 35,1627,1984

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 502 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 19,2561,1991

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 626 mg/kg

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

REFERENCE :: YHTPAD Yaoxue Tongbao. Bulletin of Pharmacology. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.13-23, 1978-88. For publisher information, see ZYZAEU. Volume(issue)/page/year: 23,182,1988

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 214 mg/kg

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

REFERENCE :: YHTPAD Yaoxue Tongbao. Bulletin of Pharmacology. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.13-23, 1978-88. For publisher information, see ZYZAEU. Volume(issue)/page/year: 23,182,1988

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1350 mg/kg

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

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 35,1627,1984

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 62500 ug/kg

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

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 35,1627,1984

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 60 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - visual field changes Behavioral - convulsions or effect on seizure threshold Kidney, Ureter, Bladder - other changes

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 19,2561,1991 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 14 gm/kg/4W-I

TOXIC EFFECTS :: Cardiac - other changes

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 35,1627,1984

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 910 mg/kg/26W-I

TOXIC EFFECTS :: Endocrine - changes in adrenal weight

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 19,2569,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 2240 mg/kg/4W-I

TOXIC EFFECTS :: Cardiac - other changes

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 35,1627,1984

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 364 mg/kg/26W-I

TOXIC EFFECTS :: Cardiac - arrhythmias (including changes in conduction) Blood - other changes

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 19,2591,1991 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 80 mg/kg

SEX/DURATION :: female 17-20 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 19,2651,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 55 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - behavioral

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 19,2635,1991

尼可地尔安全信息

[ 符号 ]:

GHS05, GHS07

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H318

[ 警示性声明 ]:
P280-P301 + P312 + P330-P305 + P351 + P338 + P310

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22-41

[ 安全声明 (欧洲) ]:
26-39

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

[ RTECS号 ]:
US4667600

[ 海关编码 ]:
2933399090

尼可地尔合成路线

详细合成路线

尼可地尔上下游产品

尼可地尔上游产品

尼可地尔下游产品

尼可地尔制备

1.6g硝酸氨乙酯硝酸盐溶于含水四氢呋喃中，加入4.3g碳酸钾溶于水的溶液后，再在0-5℃下加入3g烟酰氯盐酸盐。反应结束后，分出四氢呋喃层，处理后浓缩，加入硝酸可得1.5g硝酸尼可地尔。

或烟酰氯盐酸盐和硝酸氨乙酯，在吡啶中于5℃反应，得尼可地尔。

烟酸甲酯或其酰氯先和氨基乙醇反应后，再和浓硝酸于0～5℃成酯，可得硝酸尼可地尔。

尼可地尔海关

[ 海关编码 ]: 2933399090

[ 中文概述 ]:
2933399090. 其他结构含非稠合吡啶环的化合物. 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 ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

尼可地尔文献

Leg ulcers associated with nicorandil are possibly underdiagnosed.

Clin. Exp. Dermatol. 38(2) , 193-4, (2013)

Treating stable angina - is there a NICE way towards an international consensus?

Int. J. Clin. Pract. 66(7) , 614-8, (2012)

Peristomal ulceration caused by nicorandil.

Clin. Exp. Dermatol. 34(1) , 87-8, (2009)

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