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4-甲氧基-N,N'-二(3-吡啶甲基)-1,3-苯二甲酰胺

用途

吡考他胺是血栓素A2(TxA2)合酶和受体的联合抑制剂。吡考他胺具有抗血小板活性。Picotamide促进糖尿病患者微量白蛋白尿的减少和颈动脉斑块生长的抑制。吡考他胺可用于研究急性或慢性心血管疾病[1]。

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名称

[ CAS 号 ]:
32828-81-2

[ 中文名 ]:
匹考他胺

[ 英文名 ]:
Picotamide

[中文别名 ]:

[英文别名 ]:

EINECS 251-245-7
MFCD00866792
Plactidil
picotamide
G 137

生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 前列腺素受体

[参考文献]

[1]. Celestini A, et al. A review of picotamide in the reduction of cardiovascular events in diabetic patients. Vasc Health Risk Manag. 2007;3(1):93-98.

物理化学性质

[ 密度 ]:
1.246g/cm3

[ 沸点 ]:
668.1ºC at 760mmHg

[ 熔点 ]:
124ºC

[ 分子式 ]:
C₂₁H₂₀N₄O₃

[ 分子量 ]:
376.40900

[ 闪点 ]:
357.8ºC

[ 精确质量 ]:
376.15400

[ PSA ]:
93.21000

[ LogP ]:
3.12700

[ 折射率 ]:
1.614

MSDS

详细MSDS(安全技术说明书)

毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CZ2235500

CHEMICAL NAME :: 1,3-Benzenedicarboxamide, N,N'-bis(3-pyridinylmethyl)-4-methoxy-

CAS REGISTRY NUMBER :: 32828-81-2

BEILSTEIN REFERENCE NO. :: 0499268

LAST UPDATED :: 199612

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C21-H20-N4-O3

MOLECULAR WEIGHT :: 376.45

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 :: 3 gm/kg

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

REFERENCE :: BAXXDU British UK Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2080288

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1205 mg/kg

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

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #3973026

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 3 gm/kg

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

REFERENCE :: BAXXDU British UK Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2080288

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安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

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

[ RTECS号 ]:
CZ2235500

[ 海关编码 ]:
2933399090

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%

文献

Antivasoconstrictor and antiaggregatory activities of picotamide unrelated to thromboxane A2 antagonism.

Thromb. Haemost. 78(5) , 1385-91, (1997)

Picotamide is a dual thromboxane (Tx) A2 receptor antagonist/Tx synthase inhibitor although some observations suggest an anti-vasoconstrictor effect independent of TxA2 inhibition/antagonism. The aim ...

Determinants of fibrinogen in an Italian population suffering from claudication. Lower fibrinogen in the south compared to middle and north of Italy. The ADEP Group.

Haematologica 83(8) , 701-7, (1998)

Prospective studies have shown that high plasma levels of fibrinogen are independently associated with the risk of cardiovascular complications. In patients suffering from peripheral vascular disease ...

Thromboxane inhibition improves renal perfusion and excretory function in severe congestive heart failure.

J. Am. Coll. Cardiol. 42(1) , 133-9, (2003)

The aim of this study was to evaluate whether thromboxane inhibition can favorably affect renal perfusion and clinical conditions in patients affected by severe heart failure.The renal formation of th...

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