4205-90-7

• 常用中文名：可乐定
• 常用英文名：Clonidine
• CAS号：4205-90-7
• 分子式：C₉H₉Cl₂N₃
• 分子量：230.094
• 相关类别： 原料药 循环系统用药 抗高血压病药
• 发布时间：2018-05-29 08:00:00
• 更新时间：2024-01-02 10:39:29
• Clonidine 是一种 alpha2- 肾上腺素能激动剂,被广泛应用于麻醉研究。

名称

• 中文名: 可乐定
• 英文名: clonidine (amino form)
• 中文别名: 2-(2’,6’-二氯苯胺基)-2-咪唑啉
• 英文别名: 2,6-Dichloro-N-(imidazolidin-2-ylidene)aniline; 1H-Imidazol-2-amine, N-(2,6-dichlorophenyl)-4,5-dihydro-; Catapres-TTS; Catapresan; N-(2,6-Dichlorophenyl)-4,5-dihydro-1H-imidazol-2-amine; clonidine (amino form); 2-(2',6'-dichlorophenylamino)-imidazoline; Catapressan; [3H]-Clonidine; Clonidin; 2,6-dichloro-N-imidazolidin-2-ylidèneaniline; Catarpres; Clonidine; Catarpresan; EINECS 224-119-4; Adesipress; [14C]-Clonidine; Chlornidinum; 2,6-Dichlor-N-imidazolidin-2-ylidenanilin; Duraclon

物化性质

• 密度: 1.5±0.1 g/cm3
• 沸点: 319.3±52.0 °C at 760 mmHg
• 熔点: 141-142℃
• 分子式: C₉H₉Cl₂N₃
• 分子量: 230.094
• 闪点: 146.9±30.7 °C
• 精确质量: 229.017349
• PSA: 36.42000
• LogP: 1.41
• 蒸汽压: 0.0±0.7 mmHg at 25°C
• 折射率: 1.671
• 储存条件: 库房通风低温干燥,轻装轻卸、与氧化剂和酸类分开存放

生物活性

• 描述: Clonidine 是一种 alpha2- 肾上腺素能激动剂,被广泛应用于麻醉研究。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体
  研究领域 >> 神经疾病
• 靶点:

  alpha 2-adrenergic[1]

• 体外研究: 可乐定抑制神经元的放电活动[1]。
• 参考文献:

  [1]. Alojado ME, et al. The effect of clonidine on the activity of neurons in the rat dorsal raphe nucleus in vitro. Anesth Analg. 1994 Aug;79(2):257-60.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : NJ2487000 CHEMICAL NAME : 2-Imidazoline, 2-(2,6-dichloroanilino)- CAS REGISTRY NUMBER : 4205-90-7 LAST UPDATED : 199801 DATA ITEMS CITED : 28 MOLECULAR FORMULA : C9-H9-Cl2-N3 MOLECULAR WEIGHT : 230.11 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : Standard Draize test ROUTE OF EXPOSURE : Administration onto the skin SPECIES OBSERVED : Rodent - rabbit REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 45,257,1993 ** ACUTE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - man DOSE/DURATION : 5 ug/kg/9W-I TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) REFERENCE : EJCPAS European Journal of Clinical Pharmacology. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) V.3- 1970- Volume(issue)/page/year: 50,,463,1996 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - woman DOSE/DURATION : 30 ug/kg TOXIC EFFECTS : Behavioral - general anesthetic Cardiac - pulse rate Vascular - BP lowering not characterized in autonomic section REFERENCE : AJEMEN American Journal of Emergency Medicine. (WB Saunders, Philadelphia, PA) V.1- 1983- Volume(issue)/page/year: 14,678,1996 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - child DOSE/DURATION : 60 ug/kg TOXIC EFFECTS : Peripheral Nerve and Sensation - sensory change involving peripheral nerve Vascular - BP lowering not characterized in autonomic section Lungs, Thorax, or Respiration - respiratory depression REFERENCE : CCMDC7 Critical Care Medicine. (Williams & Wilkins, 428 E. Preston Street, Baltimore, MD 21202) V.1- 1973- Volume(issue)/page/year: 18,1124,1990 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - man DOSE/DURATION : 583 ug/kg/15W-I TOXIC EFFECTS : Kidney, Ureter, Bladder - proteinuria Endocrine - hyperglycemia REFERENCE : AJMEAZ American Journal of Medicine. (Technical Pub., 875 Third Ave., New York, NY 10022) V.1- 1946- Volume(issue)/page/year: 80,545,1986 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - man DOSE/DURATION : 2857 ng/kg TOXIC EFFECTS : Vascular - BP lowering not characterized in autonomic section REFERENCE : AIMDAP Archives of Internal Medicine. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1908- Volume(issue)/page/year: 143,2195,1983 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - man DOSE/DURATION : 43 ug/kg/10H-I TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - antipsychotic Cardiac - pulse rate REFERENCE : AEMED3 Annals of Emergency Medicine. (American College of Emergency Physicians, 1125 Executive Circle, Irving, TX 75038) Volume(issue)/page/year: 17,387,1988 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Unreported SPECIES OBSERVED : Human - woman DOSE/DURATION : 376 ug/kg/4D-I TOXIC EFFECTS : Cardiac - cardiomyopathy including infarction Cardiac - EKG changes not diagnostic of specified effects Cardiac - pulse rate REFERENCE : PEDIAU Pediatrics. (American Academy of Pediatrics, P.O. Box 1034, Evanston, IL 60204) V.1- 1948- Volume(issue)/page/year: 96,1176,1995 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Unreported SPECIES OBSERVED : Human - child DOSE/DURATION : 5 ug/kg TOXIC EFFECTS : Cardiac - cardiomyopathy including infarction Cardiac - EKG changes not diagnostic of specified effects Cardiac - pulse rate REFERENCE : PEDIAU Pediatrics. (American Academy of Pediatrics, P.O. Box 1034, Evanston, IL 60204) V.1- 1948- Volume(issue)/page/year: 96,1176,1995 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 67300 ug/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: #4389403 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Administration onto the skin SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >70 mg/kg TOXIC EFFECTS : Sense Organs and Special Senses (Olfaction) - effect, not otherwise specified Sense Organs and Special Senses (Eye) - chromodacryorrhea Sense Organs and Special Senses (Eye) - effect, not otherwise specified REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 45,257,1993 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 88400 ug/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - chromodacryorrhea Behavioral - tremor Behavioral - ataxia 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: 26,4835,1992 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 108 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - ataxia Skin and Appendages - hair 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: 18,366,1987 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 108 mg/kg TOXIC EFFECTS : Behavioral - tremor Behavioral - ataxia Skin and Appendages - hair 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: 18,366,1987 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 364 mg/kg TOXIC EFFECTS : Behavioral - tremor Behavioral - ataxia Skin and Appendages - hair 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: 18,366,1987 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 180 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : CSLNX* U.S. Army Armament Research & Development Command, Chemical Systems Laboratory, NIOSH Exchange Chemicals. (Aberdeen Proving Ground, MD 21010) Volume(issue)/page/year: NX#01892 TYPE OF TEST : LD - Lethal dose ROUTE OF EXPOSURE : Administration onto the skin SPECIES OBSERVED : Mammal - dog DOSE/DURATION : >20 mg/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Blood - changes in leukocyte (WBC) count REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 48,321,1994 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 15 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea Lungs, Thorax, or Respiration - cyanosis REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 45,249,1993 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Mammal - species unspecified DOSE/DURATION : 102 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 35,693,1985 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 2100 ug/kg/7D-I TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - lacrimation Sense Organs and Special Senses (Eye) - effect, not otherwise specified REFERENCE : ARTODN Archives of Toxicology. (Springer-Verlag, Heidelberger Pl. 3, D-1000 Berlin 33, Fed. Rep. Ger.) V.32- 1974- Volume(issue)/page/year: 41,89,1978 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Administration onto the skin SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 2275 mg/kg/13W-I TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - corneal damage Kidney, Ureter, Bladder - other changes in urine composition Related to Chronic Data - changes in prostate weight REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 45,257,1993 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 9100 ug/kg/13W-I TOXIC EFFECTS : Blood - pigmented or nucleated red blood cells Blood - other changes Blood - changes in erythrocyte (RBC) count 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: 26,4843,1992 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Administration onto the skin SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 900 mg/kg/90D-I TOXIC EFFECTS : Endocrine - hyperglycemia Blood - normocytic anemia Blood - changes in platelet count REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 48,329,1994 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 2100 mg/kg SEX/DURATION : female 1-21 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - other postnatal measures or effects REFERENCE : NETEEC Neurotoxicology and Teratology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.9- 1987- Volume(issue)/page/year: 12,359,1990 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 2080 ug/kg SEX/DURATION : female 8-20 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) REFERENCE : NRTXDN Neurotoxicology. (Intox Press, Inc., POB 34075, Little Rock, AR 72203) V.1- 1979- Volume(issue)/page/year: 9,559,1988 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 20 mg/kg SEX/DURATION : female 11 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) REFERENCE : TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 32,19A,1985 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 10 mg/kg SEX/DURATION : female 11 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) REFERENCE : TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 32,19A,1985 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X6223 No. of Facilities: 9 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 339 (estimated) No. of Female Employees: 170 (estimated)

安全

• 符号: GHS06
• 信号词: Danger
• 危害声明: H301
• 警示性声明: Missing Phrase - N15.00950417
• 危害码 (欧洲): F,T
• 风险声明 (欧洲): 11-23/24/25-39/23/24/25
• 安全声明 (欧洲): 16-36/37-45
• 危险品运输编码: UN 2811 6.1 / PGIII
• 海关编码: 2933290090

合成路线

57647-79-7 ~% 4205-90-7

文献：Chemie Linz Aktiengesellschaft Patent: US3988345 A1, 1976 ;

87-69-4 57647-79-7 ~% 4205-90-7

文献：Chemie Linz Aktiengesellschaft Patent: US3988345 A1, 1976 ;

141-43-5 57647-79-7 ~% 4205-90-7

文献：Chemie Linz Aktiengesellschaft Patent: US3988345 A1, 1976 ;

111225-65-1 107-15-3 ~90% 4205-90-7

文献：Mohanazadeh, Farajollah; Nami, Navabe; Hosseini, Samine Sadat Chinese Journal of Chemistry, 2011 , vol. 29, # 5 p. 1055 - 1058

上下游产品

上游产品  5
57647-79-7 87-69-4 141-43-5 111225-65-1
107-15-3
下游产品  1
33178-86-8

制备

【方法一】
由2,6-二氯苯胺经甲酰化、氯化、环合而得。将所得可乐定与无水乙醇及活性炭一起搅拌，加热回流，滤除活性炭，滤液加入氯化氢乙醇溶液中成盐，冷却结晶，过滤，用无水乙醇洗结晶，干燥，得可乐定盐酸盐。

海关

海关编码	2933290090
中文概述	2933290090. 其他结构含非稠合咪唑环的化合物. 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:20.0%
申报要素	品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期
Summary	2933290090. other compounds containing an unfused imidazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%