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阿折地平

阿折地平用途

Azelnidipine(CS 905; Calblock)是二氢吡啶衍生物,为L型钙离子通道阻断剂,可抗高血压。

阿折地平名称

[ CAS 号 ]:
123524-52-7

[ 中文名 ]:
阿折地平

[ 英文名 ]:
Azelnidipine

[中文别名 ]:

阿折地坪

[英文别名 ]:

Azelnidipine
UNII:PV23P19YUG
MFCD00865803

阿折地平生物活性

[ 描述 ]:

Azelnidipine(CS 905; Calblock)是二氢吡啶衍生物,为L型钙离子通道阻断剂,可抗高血压。

[ 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]. Komoda H, Inoue T, Node K. Anti-inflammatory properties of azelnidipine, a dihydropyridine-based calcium channel blocker. Clin Exp Hypertens. 2010 Jan;32(2):121-8.

[2]. Kain V, Kumar S, Sitasawad SL. Azelnidipine prevents cardiac dysfunction in streptozotocin-diabetic rats by reducing intracellular calcium accumulation, oxidative stress and apoptosis. Cardiovasc Diabetol. 2011 Nov 4;10:97.

[3]. Takano Y, Ueyama T, Ishikura F. Azelnidipine, unique calcium channel blocker could prevent stress-induced cardiac dysfunction like α·β blocker. J Cardiol. 2012 Jul;60(1):18-22.

[4]. Shimizu T, Tanaka T, Iso T et al. Azelnidipine inhibits MSX2-dependent osteogenic differentiation and matrix mineralization of vascular smooth muscle cells. Int Heart J. 2012;53(5):331-5.

[5]. Ohyama T, Sato K, Kishimoto K et al. Azelnidipine is a calcium blocker that attenuates liver fibrosis and may increase antioxidant defence. Br J Pharmacol. 2012 Feb;165(4b):1173-87.

[相关活性小分子]

阿折地平物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
709.3±60.0 °C at 760 mmHg

[ 熔点 ]:
120-126ºC

[ 分子式 ]:
C₃₃H₃₄N₄O₆

[ 分子量 ]:
582.646

[ 闪点 ]:
382.8±32.9 °C

[ 精确质量 ]:
582.247864

[ PSA ]:
139.71000

[ LogP ]:
4.21

[ 外观性状 ]:
淡黄色粉末

[ 蒸汽压 ]:
0.0±2.3 mmHg at 25°C

[ 折射率 ]:
1.659

[ 储存条件 ]:
Room temp

[ 水溶解性 ]:
水溶性：不溶；易溶于：丙酮,二甲基甲酰胺；可溶于：甲醇,乙醇

阿折地平MSDS

详细MSDS(安全技术说明书)

阿折地平毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: US7968332

CHEMICAL NAME :: 3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2-amino-6-methyl-4-(3-nitrophenyl)-, 3-(1-(diphenylmethyl)-3-azetidinyl)-5-(1-methylethyl) esster, (+-)-

CAS REGISTRY NUMBER :: 123524-52-7

LAST UPDATED :: 199803

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C33-H34-N4-O6

MOLECULAR WEIGHT :: 582.71

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3640 mg/kg/1Y-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - urine volume increased Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Nutritional and Gross Metabolic - changes in chlorine

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: 25,1757,1997

阿折地平安全信息

[ 符号 ]:

GHS05, GHS07

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H318

[ 警示性声明 ]:
P280-P305 + P351 + P338

[ 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) ]:
R22

[ 安全声明 (欧洲) ]:
26-39

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

[ RTECS号 ]:
US7968332

[ 海关编码 ]:
2933990090

阿折地平海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮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, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

阿折地平文献

Anti-atherogenic effects of the combination therapy with olmesartan and azelnidipine in diabetic apolipoprotein E-deficient mice.

Tohoku J. Exp. Med. 228 , 305-315, (2012)

Many studies have aimed to identify anti-atherogenic agents in cardiovascular medicine. We have recently demonstrated that the combination therapy with olmesartan (OLM), an angiotensin II receptor blo...

The pharmacological differences in antianginal effects of long-lasting calcium channel blockers: azelnidipine and amlodipine.

J. Cardiovasc. Pharmacol. 61(1) , 63-9, (2013)

We examined antianginal effects of azelnidipine and amlodipine in an arginine vasopressin-induced rat anginal model. Oral administration of azelnidipine or amlodipine produced long lasting inhibition ...

Azelnidipine prevents cardiac dysfunction in streptozotocin-diabetic rats by reducing intracellular calcium accumulation, oxidative stress and apoptosis.

Cardiovasc. Diabetol. 10 , 97, (2011)

Numerous evidences suggest that diabetic heart is characterized by compromised ventricular contraction and prolonged relaxation attributable to multiple causative factors including calcium accumulatio...

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