54143-56-5

• 常用中文名：醋酸氟卡胺
• 常用英文名：flecainide acetate
• CAS号：54143-56-5
• 分子式：C₁₉H₂₄F₆N₂O₅
• 分子量：474.395
• 相关类别： 原料药 循环系统用药 抗心律失常药
• 发布时间：2018-10-01 12:38:20
• 更新时间：2024-01-05 17:38:19
• Flecainide(Tambocor)能阻断位于心脏的Nav1.5钠离子通道,能抗心律失常。

名称

• 中文名: 醋酸氟卡尼
• 英文名: flecainide acetate
• 中文别名: 乙酸氟卡尼; 醋酸氟卡胺
• 英文别名: FLECAINIDE MONOACETATE; acetic acid,N-(piperidin-2-ylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide; R 818; Flecainide acetate salt; acide acétique - N-(pipéridin-2-ylméthyl)-2,5-bis(2,2,2-trifluoroéthoxy)benzamide (1:1); N-(Piperidin-2-ylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide acetate (1:1); EINECS 258-997-5; Flecainide acetate; N-(2-Piperidinylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide acetate (1:1); N-(2-Piperidylmethyl)-2,5-bis-(2,2,2-trifluoroethoxy)benzamide acetate salt; UNII:M8U465Q1WQ; N-(piperidin-2-ylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide acetate; Benzamide, N-(2-piperidinylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)-, acetate (1:1); N-(Piperidin-2-ylmethyl)-2,5-bis(2,2,2-trifluorethoxy)benzolcarboxamidacetat; Flecainide (acetate)

物化性质

• 密度: 1.286g/cm3
• 沸点: 434.9ºC at 760mmHg
• 熔点: 145-147℃
• 分子式: C₁₉H₂₄F₆N₂O₅
• 分子量: 474.395
• 闪点: 216.8ºC
• 精确质量: 474.158936
• PSA: 96.89000
• LogP: 4.25130
• 储存条件: 2-8°C
• 水溶解性: Soluble in water and in anhydrous ethanol. It is freely soluble in dilute acetic acid and practically insoluble in dilute hydrochloric acid.

生物活性

• 描述: Flecainide(Tambocor)能阻断位于心脏的Nav1.5钠离子通道,能抗心律失常。
• 相关类别:
  信号通路 >> 跨膜转运 >> 钠通道
  研究领域 >> 心血管疾病
• 参考文献:

  [1]. Yamashita T, Nakajima T, Hamada E, Flecainide inhibits the transient outward current in atrial myocytes isolated from the rabbit heart. J Pharmacol Exp Ther. 1995 Jul;274(1):315-21.

  [2]. Desaphy JF, De Luca A, Didonna MP, Different flecainide sensitivity of hNav1.4 channels and myotonic mutants explained by state-dependent block. J Physiol. 2004 Jan 15;554(Pt 2):321-34.

  [3]. Kohli V. Oral flecainide is effective in management of refractory tachycardia in infants. Indian Heart J. 2013 Mar-Apr;65(2):168-71.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : CV5792550 CHEMICAL NAME : Benzamide, N-(2-piperidinylmethyl)-2,5-bis(2,2,2-trifluoroethoxy )-, monoacetate CAS REGISTRY NUMBER : 54143-56-5 LAST UPDATED : 199606 DATA ITEMS CITED : 24 MOLECULAR FORMULA : C17-H20-F6-N2-O3.C2-H4-O2 MOLECULAR WEIGHT : 474.45 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - man DOSE/DURATION : 40 mg/kg/2W-I TOXIC EFFECTS : Cardiac - arrhythmias (including changes in conduction) Cardiac - pulse rate increase, without fall in BP REFERENCE : AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 111,107,1989 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - woman DOSE/DURATION : 40 mg/kg TOXIC EFFECTS : Cardiac - EKG changes not diagnostic of specified effects Cardiac - pulse rate increase, without fall in BP Vascular - BP lowering not characterized in autonomic section REFERENCE : BJCPAT British Journal of Clinical Practice. (Medical News Group, 1 Bedford St., London WC2E 9HD, UK) V.10(10)- 1956- Volume(issue)/page/year: 49,218,1995 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - woman DOSE/DURATION : 28 mg/kg/1W-I TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - optic nerve neuropathy REFERENCE : BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 291,450,1985 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - woman DOSE/DURATION : 160 mg/kg TOXIC EFFECTS : Cardiac - arrhythmias (including changes in conduction) Cardiac - change in rate REFERENCE : MJAUAJ Medical Journal of Australia. (Australasian Medical Pub. Co. Ltd., 71-79 Arundel St., Glebe, N.S.W., Australia) V.1- 1914- Volume(issue)/page/year: 155,349,1991 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - woman DOSE/DURATION : 56 mg/kg/1W-I TOXIC EFFECTS : Cardiac - other changes REFERENCE : AJCDAG American Journal of Cardiology. (Technical Pub. Co., 875 Third Ave., New York, NY 10022) V.1- 1958- Volume(issue)/page/year: 55,1643,1985 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - woman DOSE/DURATION : 76 mg/kg TOXIC EFFECTS : Cardiac - pulse rate increase, without fall in BP REFERENCE : AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 106,807,1987 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Human - man DOSE/DURATION : 1714 ug/kg/4M-C TOXIC EFFECTS : Cardiac - arrhythmias (including changes in conduction) REFERENCE : AHJOA2 American Heart Journal. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63146) V.1- 1925- Volume(issue)/page/year: 107,222,1984 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Multiple routes SPECIES OBSERVED : Human - man DOSE/DURATION : 26 mg/kg/89H-I TOXIC EFFECTS : Behavioral - hallucinations, distorted perceptions REFERENCE : PGMJAO Postgraduate Medical Journal. (Blackwell Scientific Pub. Ltd., POB 88, Oxford, UK) V.1- 1925- Volume(issue)/page/year: 62,61,1986 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Multiple routes SPECIES OBSERVED : Human - man DOSE/DURATION : 25 mg/kg/1W-I TOXIC EFFECTS : Cardiac - arrhythmias (including changes in conduction) REFERENCE : AJCDAG American Journal of Cardiology. (Technical Pub. Co., 875 Third Ave., New York, NY 10022) V.1- 1958- Volume(issue)/page/year: 53,329,1984 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1346 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: 22,967,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 215 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: 22,967,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 16200 ug/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: 22,967,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 170 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: 22,967,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 188 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: 22,967,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 23800 ug/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: 22,967,1991 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 22 gm/kg/2Y-C TOXIC EFFECTS : Cardiac - changes in heart weight Kidney, Ureter, Bladder - incontinence Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 73,232,1984 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 4740 mg/kg SEX/DURATION : male 64 day(s) pre-mating female 1-15 day(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - menstrual cycle changes or disorders Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) 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: 23,1785,1989 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 660 mg/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - other developmental abnormalities 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: 23,1797,1989 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 660 mg/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - other effects Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) 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: 23,1797,1989 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 1560 mg/kg SEX/DURATION : female 17-22 day(s) after conception lactating female 20 day(s) post-birth TOXIC EFFECTS : Reproductive - Maternal Effects - parturition Reproductive - Maternal Effects - postpartum Reproductive - Effects on Newborn - live birth index (measured after birth) 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: 23,1823,1989 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 780 mg/kg SEX/DURATION : female 17-22 day(s) after conception lactating female 20 day(s) post-birth TOXIC EFFECTS : Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - physical 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: 23,1823,1989 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 520 mg/kg SEX/DURATION : female 6-18 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) 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: 23,1815,1989 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 130 mg/kg SEX/DURATION : female 6-18 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) 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: 23,1815,1989 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 390 mg/kg SEX/DURATION : female 6-18 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - musculoskeletal system 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: 23,1815,1989

安全

• 符号: GHS07, GHS08
• 信号词: Danger
• 危害声明: H302-H315-H319-H335-H360
• 警示性声明: P201-P280-P301 + P312 + P330-P305 + P351 + P338-P308 + P313
• 危害码 (欧洲): Xn
• 风险声明 (欧洲): R22
• 安全声明 (欧洲): 22-26-36/37/39-45
• 危险品运输编码: UN 3249
• WGK德国: -
• RTECS号: CV5792550
• 包装等级: III
• 危险类别: 6.1(b)

合成路线

57415-36-8 64-19-7 ~87% 54143-56-5

文献："Joint Stock Company Grindeks" Patent: EP1918280 A1, 2008 ; Location in patent: Page/Page column 4; 8 ;

57415-36-8 ~87% 54143-56-5

文献：Geneva Pharmaceuticals, Inc. Patent: US6458957 B1, 2002 ;

54143-55-4 64-19-7 ~87% 54143-56-5

文献：Wang, Zhi-Xian; Li, Yuanqiang; Guntoori, Bhaskar Reddy Patent: US2005/59825 A1, 2005 ; Location in patent: Page/Page column 4 ;

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