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2-氨基-N-(2,6-二甲基苯基)丙酰胺

2-氨基-N-(2,6-二甲基苯基)丙酰胺用途

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]。

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2-氨基-N-(2,6-二甲基苯基)丙酰胺名称

[ CAS 号 ]:
41708-72-9

[ 中文名 ]:
妥卡尼

[ 英文名 ]:
Tocainide

[中文别名 ]:

[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

2-氨基-N-(2,6-二甲基苯基)丙酰胺生物活性

[ 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.

2-氨基-N-(2,6-二甲基苯基)丙酰胺物理化学性质

[ 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

2-氨基-N-(2,6-二甲基苯基)丙酰胺毒性和生态

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

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2-氨基-N-(2,6-二甲基苯基)丙酰胺安全信息

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 海关编码 ]:
2924299090

2-氨基-N-(2,6-二甲基苯基)丙酰胺合成路线

详细合成路线

2-氨基-N-(2,6-二甲基苯基)丙酰胺海关

[ 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%