41708-72-9

• 常用中文名：2-氨基-N-(2,6-二甲基苯基)丙酰胺
• 常用英文名：Tocainide
• CAS号：41708-72-9
• 分子式：C₁₁H₁₆N₂O
• 分子量：192.25800
• 相关类别： 原料药 循环系统用药 抗心律失常药
• 发布时间：2018-05-15 08:00:00
• 更新时间：2024-01-06 18:25:09
• 盐酸托可奈德是一种口服活性钠通道阻滞剂,它可以阻断神经膜上疼痛产生部位的钠通道。盐酸托可奈德是利多卡因的伯胺类似物,可用于治疗耳鸣[1][2]。

名称

• 中文名: 妥卡尼
• 英文名: tocainide
• 中文别名: 氨酰甲苯胺; 2-氨基-N-(2,6-二甲基苯基)丙酰胺
• 英文别名: R/S-Tocainide; 2-amino-2',6'-propionoxylidide; MFCD00072010; EINECS 255-505-0; TOCAINIDE; 6'-propionoxylidide,2-amino-2; alanyl-2,6-xylidide

物化性质

• 分子式: C₁₁H₁₆N₂O
• 分子量: 192.25800
• 精确质量: 192.12600
• PSA: 55.12000
• LogP: 2.36240
• 储存条件: 2-8°C

生物活性

• 描述: 盐酸托可奈德是一种口服活性钠通道阻滞剂,它可以阻断神经膜上疼痛产生部位的钠通道。盐酸托可奈德是利多卡因的伯胺类似物,可用于治疗耳鸣[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
• 靶点:

  IC50: sodium channel[1]

• 体内研究: 托卡奈德(100 mg/kg)可有效抑制冠状动脉闭塞未麻醉犬的心室异位活动。在洋地黄毒性和冠状动脉闭塞模型中终止托卡尼特输注可导致心室异位活动迅速恢复[1]。
• 参考文献:

  [1]. Alpert JS, et al. Chemistry, pharmacology, antiarrhythmic efficacy and adverse effects of tocainide hydrochloride, an orally active structural analog of lidocaine. Pharmacotherapy. 1983 Nov-Dec;3(6):316-23.

  [2]. De Luca A,et al.Optimal requirements for high affinity and use-dependent block of skeletal muscle sodium channel by N-benzyl analogs of tocainide-like compounds.Mol Pharmacol. 2003 Oct;64(4):932-45.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : UG6305000 CHEMICAL NAME : 2',6'-Propionoxylidide, 2-amino- CAS REGISTRY NUMBER : 41708-72-9 LAST UPDATED : 199707 DATA ITEMS CITED : 4 MOLECULAR FORMULA : C11-H16-N2-O MOLECULAR WEIGHT : 192.29 WISWESSER LINE NOTATION : ZY1&VMR B1 F1 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - man DOSE/DURATION : 229 mg/kg TOXIC EFFECTS : Behavioral - coma Cardiac - cardiomyopathy including infarction REFERENCE : BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 288,760,1984 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human DOSE/DURATION : 5714 ug/kg TOXIC EFFECTS : Behavioral - hallucinations, distorted perceptions Gastrointestinal - nausea or vomiting REFERENCE : DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 2,141,1977 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - man DOSE/DURATION : 2606 mg/kg/11W-I TOXIC EFFECTS : Blood - aplastic anemia REFERENCE : NEJMAG New England Journal of Medicine. (Massachusetts Medical Soc., 10 Shattuck St., Boston, MA 02115) V.198- 1928- Volume(issue)/page/year: 314,583,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 94 mg/kg TOXIC EFFECTS : Peripheral Nerve and Sensation - local anesthetic Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia 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: 24,1059,1981

安全

• 危害码 (欧洲): Xn: Harmful;
• 风险声明 (欧洲): R22
• 海关编码: 2924299090

合成路线

41708-73-0 ~% 41708-72-9

文献：Astra Pharmaceutical Products, Inc. Patent: US4218477 A1, 1980 ; US 4218477 A

36292-29-2 ~% 41708-72-9

文献：Astra Pharmaceutical Products, Inc. Patent: US4218477 A1, 1980 ; US 4218477 A

71344-61-1 ~% 1445-69-8 41708-72-9

文献：Tenthorey; Block; Ronfeld; McMaster; Byrnes Journal of Medicinal Chemistry, 1981 , vol. 24, # 7 p. 798 - 806

海关

海关编码	2924299090
中文概述	2924299090. 其他环酰胺（包括环氨基甲酸酯）（包括其衍生物以及他们的盐）. 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:30.0%
申报要素	品名, 成分含量, 用途, 包装
Summary	2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%