511-13-7

• 常用中文名：盐酸氯苯达诺
• 常用英文名：2-chloro-alpha-[2-dimethylaminoethyl]benzhydrol hydrochloride
• CAS号：511-13-7
• 分子式：C₁₇H₂₁Cl₂NO
• 分子量：326.261
• 相关类别： 原料药 呼吸系统用药 镇咳药
• 发布时间：2018-06-29 22:11:06
• 更新时间：2024-01-12 22:02:33
• 盐酸氯苯二酚(氯苯达诺)是一种口服有效镇咳剂。盐酸氯苯二酚可用于研究上呼吸道感染(URI)引起的急性咳嗽[1][2]。

名称

• 中文名: 敌退咳
• 英文名: Clofedanol Hydrochloride
• 中文别名: 2-氯-alpha-[2-二甲氨基乙基]二苯甲醇盐酸盐; 1-邻氯苯基-1-苯基-3-二甲氨基丙醇盐酸盐
• 英文别名: 2-Chloro-a-(2-(dimethylamino)ethyl)benzhydrol Hydrochloride; MFCD00079013; 1-(2-Chlorophenyl)-3-(dimethylamino)-1-phenylpropan-1-ol hydrochloride (1:1); a-(2-dimethylaminoethyl)-o-chlorobenzhydrol hydrochloride; EINECS 208-124-9; Benzenemethanol, 2-chloro-α-[2-(dimethylamino)ethyl]-α-phenyl-, hydrochloride (1:1); 2-Chloro-a-(2-(dimethylamino)ethyl)-a-phenylbenzenemethanol Hydrochloride; 1-(2-chlorophenyl)-3-(dimethylamino)-1-phenylpropan-1-ol,hydrochloride; 1-(2-Chlorophenyl)-3-(dimethylamino)-1-phenyl-1-propanol hydrochloride (1:1)

物化性质

• 沸点: 429.8ºC at 760mmHg
• 分子式: C₁₇H₂₁Cl₂NO
• 分子量: 326.261
• 闪点: 213.7ºC
• 精确质量: 325.100006
• PSA: 23.47000
• LogP: 4.32960

生物活性

• 描述: 盐酸氯苯二酚(氯苯达诺)是一种口服有效镇咳剂。盐酸氯苯二酚可用于研究上呼吸道感染(URI)引起的急性咳嗽[1][2]。
• 相关类别:
  研究领域 >> 感染
  信号通路 >> 其他 >> 其他
• 体内研究: 氯苯二胺(氯苯达诺)盐酸盐(0-162 mg/kg；p.o.或s.c.；一次)可降低兔子和猫的呼吸道液体输出量[1]。动物模型：健康、成年、雄性兔子和猫[1]剂量：2.0、6.0、18、54和162 mg/kg(PO)或1.0、3.0、9.0、27和81 mg/kg(SC)给药：口服或皮下给药,一次。结果：在给药后的一到三小时内,呼吸道液体输出量略有降低,但显著降低。导致呼吸道出现粘液颗粒的动物数量减少。
• 参考文献:

  [1]. Boyd EM, et al. Chlophedianol Hydrochloride: A New Antitussive Agent. Can Med Assoc J. 1960 Dec 17;83(25):1298-301.

  [2]. Paul IM. Therapeutic options for acute cough due to upper respiratory infections in children. Lung. 2012 Feb;190(1):41-4.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : DC7600000 CHEMICAL NAME : Benzhydrol, 2-chloro-alpha-(2-(dimethylamino)ethyl)-, hydrochloride CAS REGISTRY NUMBER : 511-13-7 LAST UPDATED : 199404 DATA ITEMS CITED : 21 MOLECULAR FORMULA : C17-H20-Cl-N-O.Cl-H MOLECULAR WEIGHT : 326.29 WISWESSER LINE NOTATION : GR BXQR&2N1&1 &GH 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 : 350 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #3031377 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 295 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: 12,933,1981 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 440 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : GNRIDX Gendai no Rinsho. (Tokyo, Japan) V.1-10, 1967-76(?). Volume(issue)/page/year: 7,177,1973 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 53 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : GNRIDX Gendai no Rinsho. (Tokyo, Japan) V.1-10, 1967-76(?). Volume(issue)/page/year: 7,177,1973 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 268 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : GNRIDX Gendai no Rinsho. (Tokyo, Japan) V.1-10, 1967-76(?). Volume(issue)/page/year: 7,177,1973 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 284 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : THERAP Therapie. (Doin, Editeurs, 8, Place de l'Odeon, F-75006 Paris, France) V.1- 1946- Volume(issue)/page/year: 15,93,1960 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 130 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : GNRIDX Gendai no Rinsho. (Tokyo, Japan) V.1-10, 1967-76(?). Volume(issue)/page/year: 7,177,1973 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 95 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #3031377 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 42 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : THERAP Therapie. (Doin, Editeurs, 8, Place de l'Odeon, F-75006 Paris, France) V.1- 1946- Volume(issue)/page/year: 15,93,1960 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 84 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 32,1281,1981 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - cat DOSE/DURATION : 80 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #3031377 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : >50 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #3031377 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - guinea pig DOSE/DURATION : 130 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #3031377 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Mammal - species unspecified DOSE/DURATION : 186 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,369,1972 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 6720 mg/kg/28D-C TOXIC EFFECTS : Liver - other changes Endocrine - changes in thymus weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 9,137,1975 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 10920 mg/kg/26W-C TOXIC EFFECTS : Liver - changes in liver weight Endocrine - changes in spleen weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 9,137,1975 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 3360 mg/kg/28D-C TOXIC EFFECTS : Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 9,137,1975 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 192 mg/kg SEX/DURATION : female 9-14 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 - musculoskeletal system REFERENCE : GNRIDX Gendai no Rinsho. (Tokyo, Japan) V.1-10, 1967-76(?). Volume(issue)/page/year: 7,177,1973 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 120 mg/kg SEX/DURATION : female 7-12 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - musculoskeletal system REFERENCE : GNRIDX Gendai no Rinsho. (Tokyo, Japan) V.1-10, 1967-76(?). Volume(issue)/page/year: 7,177,1973 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 192 mg/kg SEX/DURATION : female 7-12 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) REFERENCE : GNRIDX Gendai no Rinsho. (Tokyo, Japan) V.1-10, 1967-76(?). Volume(issue)/page/year: 7,177,1973 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 83156 No. of Facilities: 819 (estimated) No. of Industries: 2 No. of Occupations: 3 No. of Employees: 1897 (estimated)

安全

• 危害码 (欧洲): T
• 风险声明 (欧洲): 25
• 安全声明 (欧洲): 36/37/39-45
• 危险品运输编码: UN 3249
• RTECS号: DC7600000
• 包装等级: III
• 危险类别: 6.1(b)

制备

【方法一】
邻氯二苯酮经加成、催化、氢化、甲基化、成盐而得。