<生产厂家价格>

尼索地平

尼索地平用途

Nisoldipine(BAY-k 5552; Sular)是高效特异的L型Cav1.2通道阻断剂,IC50为10 nM。

尼索地平名称

[ CAS 号 ]:
63675-72-9

[ 中文名 ]:
尼索地平

[ 英文名 ]:
Nisoldipine

[中文别名 ]:

布洛芬.异丁苯丙酸

[英文别名 ]:

EINECS 264-407-7
Nisoldipine
MFCD00478055
Baymycard
UNII:4I8HAB65SZ
Syscor
Zadipina

尼索地平生物活性

[ 描述 ]:

Nisoldipine(BAY-k 5552; Sular)是高效特异的L型Cav1.2通道阻断剂,IC50为10 nM。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钙通道

研究领域 >> 心血管疾病

[参考文献]

[1]. Hamilton SF, Houle LM, Thadani U. Rapid-release and coat-core formulations of nisoldipine in treatment of hypertension, angina, and heart failure. Heart Dis. 1999 Nov-Dec;1(5):279-88.

[2]. Fodor JG. Nisoldipine CC: efficacy and tolerability in hypertension and ischemic heart disease. Cardiovasc Drugs Ther. 1997 Jan;10 Suppl 3:873-9.

[3]. D.J. Duncker, J.M. Hartog, P.G. Hugenholtz, et al. The effects of nisoldipine (Bay K 5552) on cardiovascular performance and regional blood flow in pentobarbital - anaesthetized pigs with or without β-adrenoceptor blockade. British Journal of Pharmacology

[4]. Jan W. De Jong, Tom Huizer, Jan G.P. Tijssen. Energy conservation by nisoldipine in ischaemic heart. British Journal of Pharmacology. 1984, 83(4): 943-949

[相关活性小分子]

尼索地平物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
505.8±50.0 °C at 760 mmHg

[ 熔点 ]:
147-148°C

[ 分子式 ]:
C₂₀H₂₄N₂O₆

[ 分子量 ]:
388.414

[ 闪点 ]:
259.7±30.1 °C

[ 精确质量 ]:
388.163422

[ PSA ]:
110.45000

[ LogP ]:
4.38

[ 外观性状 ]:
淡黄褐色的晶体

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.544

[ 储存条件 ]:
-20°C Freezer

[ 水溶解性 ]:
水溶性：不溶；易溶于：二氯甲烷,丙酮；可溶于：甲醇

尼索地平MSDS

详细MSDS(安全技术说明书)

尼索地平毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: US7975600

CHEMICAL NAME :: 3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-, methyl 2-methyl propyl ester

CAS REGISTRY NUMBER :: 63675-72-9

LAST UPDATED :: 199612

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C20-H24-N2-O6

MOLECULAR WEIGHT :: 388.46

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 :: 1257 mg/kg

TOXIC EFFECTS :: Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - cyanosis Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,3285,1988

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 674 mg/kg

TOXIC EFFECTS :: Behavioral - changes in motor activity (specific assay) Skin and Appendages - hair

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,3285,1988

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1120 ug/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,3285,1988

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 411 mg/kg

TOXIC EFFECTS :: Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - cyanosis Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,3285,1988

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 384 mg/kg

TOXIC EFFECTS :: Behavioral - changes in motor activity (specific assay) Skin and Appendages - hair

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,3285,1988

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 360 ug/kg

TOXIC EFFECTS :: Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - other changes Skin and Appendages - hair

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,3285,1988

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 400 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 23,682,1992

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 2 mg/kg

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

REFERENCE :: NDADD8 New Drugs Annual: Cardiovascular Drugs. (New York, NY) V.1-2, 1983-84. For publisher information, see NCDREP. Volume(issue)/page/year: 1,243,1983

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >5 gm/kg

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

REFERENCE :: NDADD8 New Drugs Annual: Cardiovascular Drugs. (New York, NY) V.1-2, 1983-84. For publisher information, see NCDREP. Volume(issue)/page/year: 1,243,1983

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 2500 ug/kg

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

REFERENCE :: NDADD8 New Drugs Annual: Cardiovascular Drugs. (New York, NY) V.1-2, 1983-84. For publisher information, see NCDREP. Volume(issue)/page/year: 1,243,1983

尼索地平安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H312

[ 警示性声明 ]:
P280

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38:Irritating to eyes, respiratory system and skin .

[ 安全声明 (欧洲) ]:
S26-S36

[ 危险品运输编码 ]:
3077

[ WGK德国 ]:
2

[ RTECS号 ]:
3425000

[ 海关编码 ]:
2942000000

尼索地平合成路线

详细合成路线

尼索地平上下游产品

尼索地平上游产品

尼索地平下游产品

尼索地平制备

邻硝基苯甲醛先和乙酰乙酸异丁酯反应，得2-(2-硝基苯亚甲基)乙酰乙酸异丁酯。然后14.6g(50mmo1)2-(2-硝基苯亚甲基)乙酰乙酸异丁酯和5.8g(50mmo1)3-氨基丁烯酸甲酯在80ml乙醇中，加热回流20h。冷却后，减压蒸去溶剂。油状的剩余物和少量的乙醇混合，放置少许即完全析出结晶。过滤，再用乙醇重结晶，得15.2g尼索地平，收率78%，熔点151～152℃。

尼索地平海关

[ 海关编码 ]: 2942000000

尼索地平文献

Fast disintegrating tablets of nisoldipine for intra-oral administration.

Pharm. Dev. Technol. 19(6) , 641-50, (2014)

Nisoldipine is a calcium channel blocker with low and variable oral bioavailability. This was attributed to slow dissolution and presystemic metabolism. Accordingly, the objective of this work was to ...

Anti-arrhythmic and hemodynamic effects of oxy nifedipine, oxy nimodipine, oxy nitrendipine and oxy nisoldipine.

Pharmacol. Res. 66(4) , 300-8, (2012)

Our previous studies have established cardio-protective effects of furnidipine and its active metabolites. We therefore decided to compare the influence of oral and intravenous administration of furni...

Why is nisoldipine a specific agent in ischemic left ventricular dysfunction?

Am. J. Cardiol. 75(13) , 36E-40E, (1995)

Nisoldipine is a dihydropyridine calcium entry blocker that inhibits contraction of vascular smooth muscle with a potency that is 2-3 times greater than its impact on myocardial contractility. In isol...

更多文献