73-78-9

• 常用中文名：盐酸利多卡因
• 常用英文名：Lidocaine hydrochloride
• CAS号：73-78-9
• 分子式：C₁₄H₂₃ClN₂O
• 分子量：270.798
• 相关类别： 原料药 Anesthetic Agents Local anesthetics
• 发布时间：2018-02-03 08:00:00
• 更新时间：2024-01-01 17:38:50
• Lidocaine盐酸盐体内体外证实有抗炎症活性,可能和弱化炎症因子和ICAM1有关。

名称

• 中文名: 盐酸利多卡因
• 英文名: lidocaine hydrochloride
• 中文别名: 2-二乙氨基-N-2,6-二甲苯基乙酰胺氮盐酸盐; 利多卡因盐酸盐; 克拉维酸锂; N-(2,6-二甲苯基)-2-(二乙氨基)乙酰胺盐酸盐
• 英文别名: LIDOCAINE HCL; 2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide,hydrochloride; 2-(Diethylamino)-N-(2,6-dimethylphenyl)acetamidhydrochlorid; Xyloneural; XYLOCAINE HYDROCHLORIDE; N-(2,6-Dimethylphenyl)-N,N-diethylglycinamide hydrochloride (1:1); MFCD00034865; (Diethylamino)-2',6'-acetoxylidide Monohydrochloride; 2-(diéthylamino)-N-(2,6-diméthylphényl)acétamide chlorhydrate; Xilina hydrochloride; 2-(Diethylamino)-N-(2,6-dimethylphenyl)acetamide, hydrochloride (1:1); N-(2,6-dimethylphenyl)-N,N-diethylglycinamide hydrochloride; Lidocaine hydrochloride; lignocaine hydrochloride; 2-(Diethylamino)-N-(2,6-dimethylphenyl)acetamide monohydrochloride; Acetamide, 2-(diethylamino)-N-(2,6-dimethylphenyl)-, hydrochloride (1:1); Lidocaton; Lidothesin; Laryng-O-jet; N-(2,6-dimethylphenyl)-N2,N2-diethylglycinamide hydrochloride; 2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide hydrochloride; EINECS 200-803-8; 2',6'-Acetoxylidide, 2-(diethylamino)-, monohydrochloride (8CI); Xylocard; 2N2&1VMR B1 F1 &&HCl; Lidocaine (hydrochloride)

物化性质

• 沸点: 350.8ºC at 760 mmHg
• 熔点: 80-82°C
• 分子式: C₁₄H₂₃ClN₂O
• 分子量: 270.798
• 闪点: 166ºC
• 精确质量: 270.149902
• PSA: 32.34000
• LogP: 3.45870
• 外观性状: 白色晶体粉末
• 储存条件: Refrigerator
• 计算化学:

  1.疏水参数计算参考值（XlogP）:无

  2.氢键供体数量:2

  3.氢键受体数量:2

  4.可旋转化学键数量:5

  5.互变异构体数量:3

  6.拓扑分子极性表面积32.3

  7.重原子数量:18

  8.表面电荷:0

  9.复杂度:228

  10.同位素原子数量:0

  11.确定原子立构中心数量:0

  12.不确定原子立构中心数量:0

  13.确定化学键立构中心数量:0

  14.不确定化学键立构中心数量:0

  15.共价键单元数量:2

生物活性

• 描述: Lidocaine盐酸盐体内体外证实有抗炎症活性,可能和弱化炎症因子和ICAM1有关。
• 相关类别:
  信号通路 >> 跨膜转运 >> 钠通道
  研究领域 >> 炎症/免疫
• 参考文献:

  [1]. VAN DER Wal S, et al. Lidocaine increases the anti-inflammatory cytokine IL-10 following mechanical ventilation in healthy mice. Acta Anaesthesiol Scand. 2014 Oct 14.

  [2]. Acevedo-Arcique CM, et al. Lidocaine, dexmedetomidine and their combination reduce isoflurane minimum alveolar concentration in dogs. PLoS One. 2014 Sep 18;9(9):e106620.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : AN7600000 CHEMICAL NAME : 2',6'-Acetoxylidide, 2-(diethylamino)-, hydrochloride CAS REGISTRY NUMBER : 73-78-9 LAST UPDATED : 199712 DATA ITEMS CITED : 27 MOLECULAR FORMULA : C14-H22-N2-O.Cl-H MOLECULAR WEIGHT : 270.84 WISWESSER LINE NOTATION : 2N2&1VMR B1 F1 &GH HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : Standard Draize test ROUTE OF EXPOSURE : Administration onto the skin SPECIES OBSERVED : Rodent - rabbit REFERENCE : AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 137,410,1962 TYPE OF TEST : Standard Draize test ROUTE OF EXPOSURE : Administration into the eye SPECIES OBSERVED : Rodent - rabbit REFERENCE : AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 137,410,1962 ** ACUTE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - infant DOSE/DURATION : 1600 ug/kg/9H-I TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold REFERENCE : AEMED3 Annals of Emergency Medicine. (American College of Emergency Physicians, 1125 Executive Circle, Irving, TX 75038) Volume(issue)/page/year: 17,725,1988 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - infant DOSE/DURATION : 1632 mg/kg/1W-I TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold REFERENCE : CPEDAM Clinical Pediatrics (Philadelphia). (Lippincott/Harper, Journal Fulfillment Dept., 2350 Virginia Ave., Hagerstown, MD 21740) V.1- 1962- Volume(issue)/page/year: 22,190,1983 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Human - infant DOSE/DURATION : 10 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Behavioral - coma Lungs, Thorax, or Respiration - other changes REFERENCE : JTCTDW Journal of Toxicology, Clinical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.19- 1982- Volume(issue)/page/year: 28,101,1990 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Human - child DOSE/DURATION : 60 mg/kg/1H TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Vascular - BP lowering not characterized in autonomic section REFERENCE : JTCTDW Journal of Toxicology, Clinical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.19- 1982- Volume(issue)/page/year: 24,51,1986 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Human - man DOSE/DURATION : 9 mg/kg/4H-C TOXIC EFFECTS : Cardiac - cardiomyopathy including infarction REFERENCE : DICPBB Drug Intelligence and Clinical Pharmacy. (POB 42435, Cincinnati, OH 45242) V.3- 1969- Volume(issue)/page/year: 19,669,1985 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Human - man DOSE/DURATION : 7143 ug/kg TOXIC EFFECTS : Cardiac - pulse rate increase, without fall in BP REFERENCE : CHETBF Chest. (American College of Chest Physicians, 911 Busse Hwy, Park Ridge, IL 60068) V.57- 1970- Volume(issue)/page/year: 61,682,1972 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Implant SPECIES OBSERVED : Human - man DOSE/DURATION : 5714 ug/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold REFERENCE : CMAJAX Canadian Medical Association Journal. (Canadian Medical Assoc., POB 8650, Ottawa, ON K1G 0G8, Canada) V.1- 1911- Volume(issue)/page/year: 137,219,1987 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 122 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 111,224,1954 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 570 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : RPOBAR Research Progress in Organic-Biological and Medicinal Chemistry. (New York, NY) V.1-3, 1964-72. Discontinued. Volume(issue)/page/year: 2,299,1970 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 21 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : RPOBAR Research Progress in Organic-Biological and Medicinal Chemistry. (New York, NY) V.1-3, 1964-72. Discontinued. Volume(issue)/page/year: 2,299,1970 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 220 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : RPOBAR Research Progress in Organic-Biological and Medicinal Chemistry. (New York, NY) V.1-3, 1964-72. Discontinued. Volume(issue)/page/year: 2,299,1970 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 63 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 274,253,1985 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 163 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 103,353,1960 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 15 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory stimulation REFERENCE : JPPMAB Journal of Pharmacy and Pharmacology. (Pharmaceutical Soc. of Great Britain, 1 Lambeth High St., London SEI 7JN, UK) V.1- 1949- Volume(issue)/page/year: 14,48T,1962 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 177 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : DDREDK Drug Development Research. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1981- Volume(issue)/page/year: 21,277,1990 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 65700 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JNPHAG Journal de Pharmacologie. (SPPIF, B.P.22, F-41353 Vineuil, France) V.1- 1970- Volume(issue)/page/year: 2,240,1971 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 25600 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,879,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intratracheal SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 28 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 200,359,1972 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - guinea pig DOSE/DURATION : 24500 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 113,313,1958 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Parenteral SPECIES OBSERVED : Amphibian - frog DOSE/DURATION : 159 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 289,278,1987 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Implant DOSE : 7500 mg/kg SEX/DURATION : female 3-17 day(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - parturition Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system REFERENCE : ANESAV Anesthesiology. (Lippincott/Harper, Journal Fulfillment Dept., 2350 Virginia Ave., Hagerstown, MD 21740) V.1- 1940- Volume(issue)/page/year: 65,626,1986 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 83491 No. of Facilities: 397 (estimated) No. of Industries: 3 No. of Occupations: 5 No. of Employees: 13412 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 83491 No. of Facilities: 1385 (estimated) No. of Industries: 6 No. of Occupations: 17 No. of Employees: 68071 (estimated) No. of Female Employees: 56919 (estimated)

安全

• 危险品运输编码: 3249
• 包装等级: III
• 危险类别: 6.1(b)
• 海关编码: 2924299090

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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%