88069-49-2

• 常用中文名：盐酸吡西卡呢
• 常用英文名：Pilsicainide hydrochloride
• CAS号：88069-49-2
• 分子式：C₁₇H₂₄N₂O
• 分子量：326.862
• 相关类别： 原料药 循环系统用药 抗心律失常药
• 发布时间：2018-05-18 08:00:00
• 更新时间：2024-01-08 12:23:35
• 盐酸吡西卡尼(SUN-1165)是一种口服活性钠通道阻滞剂和有效的Ic类抗心律失常药[1][2]。

名称

• 中文名: 盐酸吡西卡尼
• 英文名: N-(2,6-dimethylphenyl)-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-yl)acetamide,hydrochloride
• 中文别名: N-(2,6-二甲基苯基)-2-(1,2,3,5,6,7-六氢吡咯烷嗪-8-基)乙酰胺盐酸盐; 盐酸吡西卡呢
• 英文别名: N-(2,6-Dimethylphenyl)-2-(tetrahydro-1H-pyrrolizin-7a(5H)-yl)acetamide hydrochloride hydrate; Sunrythm; Pilsicainide HCl; 1H-Pyrrolizine-7a(5H)-acetamide,N-(2,6-dimethylphenyl)tetrahydro-,monohydrochloride; Sunrythm(R); N-(2,6-dimethylphenyl)-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-yl)acetamide hydrochloride; Pilsicainide hydrochloride; N-(2,6-dimethylphenyl)-8-pyrrolizidineacetamide hydrochloride hemihydrate; 1H-Pyrrolizine-7a(5H)-acetamide, N-(2,6-dimethylphenyl)tetrahydro-, hydrochloride, hydrate (1:1:1); Tetrahydro-N-(2,6-dimethylphenyl)-1H-pyrrolizine-7a(5H)-acetamide hydrochloride hemihydrate; SUN 1165; N-(2,6-Dimethylphenyl)-1H-pyrrolizine-8-acetamide hydrochloride; Pilsicainide Hydrochloride Hemihydrate; N-(2,6-Dimethylphenyl)-8-pyrrolizidineacetamide monohydrochloride; 1H-Pyrrolizine-8-acetamide,hexahydro-N-(2,6-dimethylphenyl)-,hydrochloride

物化性质

• 沸点: 416.9ºC at 760 mmHg
• 熔点: 212-214°
• 分子式: C₁₇H₂₄N₂O
• 分子量: 326.862
• 闪点: 205.9ºC
• 精确质量: 326.176117
• PSA: 32.34000
• LogP: 3.27130
• 储存条件: 2-8°C

生物活性

• 描述: 盐酸吡西卡尼(SUN-1165)是一种口服活性钠通道阻滞剂和有效的Ic类抗心律失常药[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: 盐酸吡西卡因(SUN-1165)(10-200μg/mL)以剂量依赖性方式降低净内向电流的峰值幅度,在左旋甲状腺素(T4)处理的大鼠心房细胞中IC50为29.2±22.9μg/mL[1]。
• 体内研究: 盐酸吡西卡因(SUN-1165)(2 mg/kg；静脉注射；一次)通过降低最大dV/dt和净内向电流降低T4处理大鼠心房的传导速度[1]。动物模型：雄性Sprague-Dawley(SD)大鼠,体重200-220 g,给予左旋甲状腺素(T4)治疗[1]剂量：2 mg/kg给药：在2分钟内向右侧颈外静脉推注,一次结果：结果：给药后15和60分钟QT间期显著延长。P波和QRS波群持续时间显著缩短。显著降低动作电位幅度(APA)和最大dV/dt,并显著延长动作电位持续时间。
• 参考文献:

  [1]. Yamakawa M, et al. Effect of sodium channel blocker, pilsicainide hydrochloride, on net inward current of atrial myocytes in thyroid hormone toxicosis rats. Thyroid. 2005 Jul;15(7):653-9.

  [2]. Plosker GL. Pilsicainide. Drugs. 2010 Mar 5;70(4):455-67.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : UY7758200 CAS REGISTRY NUMBER : 88069-49-2 LAST UPDATED : 199712 DATA ITEMS CITED : 14 MOLECULAR FORMULA : C17-H24-N2-O.Cl-H.1/2H2-O MOLECULAR WEIGHT : 317.86 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 : Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,457,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 105 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,457,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 18 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,457,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 175 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,457,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 85 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,457,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 410 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 28,714,1985 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 17 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,457,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 50 mg/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - tremor Behavioral - changes in motor activity (specific assay) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 38,1398,1988 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 18 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Cardiac - other changes Lungs, Thorax, or Respiration - respiratory depression REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,461,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 87 mg/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - tremor Behavioral - changes in motor activity (specific assay) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 38,1398,1988 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 14560 mg/kg/13W-I TOXIC EFFECTS : Behavioral - food intake (animal) Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,469,1991 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 252 mg/kg/4W-I TOXIC EFFECTS : Lungs, Thorax, or Respiration - respiratory stimulation Related to Chronic Data - death REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 54,1,1997 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 2730 mg/kg/13W-I TOXIC EFFECTS : Cardiac - other changes Related to Chronic Data - death REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,485,1991 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 168 mg/kg/4W-I TOXIC EFFECTS : Related to Chronic Data - death REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 54,1,1997

安全

• 危害码 (欧洲): Xi
• 海关编码: 2933990090

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%