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吡西卡尼

吡西卡尼用途

吡西卡肽(SUN 1165游离酸)是一种强效钠通道阻滞剂和强效Ic类抗心律失常剂[1][2]。

吡西卡尼名称

[ CAS 号 ]:
88069-67-4

[ 中文名 ]:
吡西卡尼

[ 英文名 ]:
pilsicainide

[中文别名 ]:

[英文别名 ]:

Pilzicainide
Pilsicainide HCl
Pilsicainida [INN-Spanish]
n-(2,6-dimethylphenyl)-8-pyrrolizidineacetamide
Pilsicainidum [INN-Latin]
Pilsicainide
Pilsicainide [INN]

吡西卡尼生物活性

[ 描述 ]:

吡西卡肽(SUN 1165游离酸)是一种强效钠通道阻滞剂和强效Ic类抗心律失常剂[1][2]。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钠通道

研究领域 >> 心血管疾病

[体外研究]

吡西甲酰亚胺(SUN 1165游离酸；10-200μg/mL)以剂量依赖性方式降低左甲状腺素(T4)处理的大鼠心房细胞中净内向电流的峰值振幅,IC50为29.2μg/mL[1]。

[体内研究]

吡西卡肽(SUN 1165游离酸；2 mg/kg；静脉注射；一次)通过降低最大dV/dt和净向内电流来降低T4治疗大鼠心房的传导速度[1]。动物模型：雄性Sprague-Dawley(SD)大鼠,体重200-220g,接受左旋甲状腺素(T4)治疗[1]剂量：2mg/kg给药：在2分钟内向右颈外静脉注射一次。结果：给药后15和60分钟延长QT间期。缩短P波和QRS波持续时间。动作电位振幅(APA)和最大dV/dt显著降低,动作电位持续时间显著延长。

吡西卡尼物理化学性质

[ 密度 ]:
1.11 g/cm3

[ 沸点 ]:
416.9ºC at 760 mmHg

[ 分子式 ]:
C₁₇H₂₄N₂O

[ 分子量 ]:
272.38500

[ 精确质量 ]:
272.18900

[ PSA ]:
32.34000

[ LogP ]:
3.27130

[ 折射率 ]:
1.581

[ 储存条件 ]:
room temp

吡西卡尼毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UY7758100

CHEMICAL NAME :: 1H-Pyrrolizine-7a(5H)-acetamide, tetrahydro-N-(2,6-dimethylphenyl)-, hydrochloride, hemihydrate

CAS REGISTRY NUMBER :: 88069-67-4

LAST UPDATED :: 199404

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C17-H24-N2-O.Cl-H.1/2H2-O

MOLECULAR WEIGHT :: 317.88

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 :: 255 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: 22,769,1991

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 105 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: 22,769,1991

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 18 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: 22,769,1991

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 175 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: 22,769,1991

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 85 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: 22,769,1991

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 17 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: 22,769,1991

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 53 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: 22,769,1991

吡西卡尼安全信息

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22

[ 海关编码 ]:
2933990090

吡西卡尼合成路线

详细合成路线

吡西卡尼上下游产品

吡西卡尼上游产品

吡西卡尼下游产品

吡西卡尼制备

四氢双稠吡咯乙酸乙酯和2，6-二甲基苯胺在氢化钠作用下，在二氧六环中于100℃加热缩合，可得吡西卡尼。也可将四氢双稠吡咯乙酸乙酯水解，再氯化成四氢双稠吡咯乙酰氯，然后和2，6-二甲基苯胺缩合。

吡西卡尼海关

[ 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%