N-(2,6-Dichlorophenyl)-4,5-dihydro-1H-imidazol-2-amine N-(2,6-二氯苯基)-4,5-二氢-1H-咪唑-2-胺
CAS 4205-90-7 MFCD04205907
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相关文献及参考
- [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.
安全信息
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 : 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 : 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
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
TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat 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 SPECIES OBSERVED : Rodent - mouse 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 SPECIES OBSERVED : Rodent - mouse DOSE : 10 mg/kg SEX/DURATION : female 11 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) REFERENCE : TJAD
TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat 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
- H301 Toxic if swallowed 吞食有毒
- H310 Fatal in contact with skin 皮肤接触致命
- H330 Fatal if inhaled 吸入致命
- P260 Do not breathe dust/fume/gas/mist/vapours/spray. 不要吸入粉尘/烟/气体/烟雾/蒸汽/喷雾。
- P262 Do not get in eyes, on skin, or on clothing. 不要接触眼睛,皮肤或衣服。
- P264 Wash hands thoroughly after handling. 处理后要彻底洗净双手。
- P270 Do not eat, drink or smoke when using this product. 使用本产品时不要吃东西,喝水或吸烟。
- P271 Use only outdoors or in a well-ventilated area.? 只能在室外或通风良好的地方使用。
- P280 Wear protective gloves/protective clothing/eye protection/face protection. 戴防护手套/防护服/眼睛的保护物/面部保护物。
- P284 Wear respiratory protection.? 佩戴呼吸保护装置。
- P301+P310
- P301+P316
- P302+P350
- P302+P352
- P304+P340
- P310 Immediately call a POISON CENTER or doctor/physician. 立即呼救解毒中心或医生/医师。
- P316
- P320 Specific treatment is urgent (see … on this label). 紧急具体治疗(见本标签上的)。
- P321 Specific treatment (see … on this label). 具体治疗(见本标签上的)。
- P322 Specific measures (see …on this label). 具体治疗(见本标签上的)。
- P330 Rinse mouth. 漱口
- P361 Remove/Take off immediately all contaminated clothing. 立即去除/脱掉所有被污染的衣服。
- P361+P364
- P363 Wash contaminated clothing before reuse. 被污染的衣服洗净后方可重新使用。
- P403+P233
- P405 Store locked up. 上锁保管。
- P501 Dispose of contents/container to..… 处理内容物/容器.....
其他信息
- 药理作用:盐酸可乐定为中枢性降压药,能激活血管运动中枢α2受体,引起外周交感神经抑制,导致血管扩张,使心输出量减少,心率减慢,血压下降。并能明显减少肾素分泌,作用强于甲基多巴。服药后30分钟有效,可维持6~8小时。常见商品名为血压得平、氯压定、可乐宁、可乐定,适用于治疗中度及重度高血压,亦可治偏头痛、绝经期潮热、痛经、戒绝阿片瘾毒症状。 美国食品药物管理局(FDA)已经批准盐酸可乐定缓释片(规格0.1mg和0.2mg)单用或联合兴奋剂用于治疗6岁至17岁的注意力缺陷多动症(ADHD)患儿。
- 类别:有毒物质
- 可燃性危险特性:明火、受热、氧化剂可燃; 燃烧排放有毒氯化物和氮氧化物烟雾
- 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。
- 灭火剂:雾状水、泡沫、砂土、二氧化碳、1211灭火剂
- 急性毒性:口服- 大鼠 LD50 67.3 毫克/ 公斤; 口服- 小鼠 LD50: 108 毫克/公斤
- 不良反应:常见:最常见口干(与剂量有关),昏睡,头晕,精神抑郁,便秘和镇静,性功能降低和夜尿多,瘙痒,恶心、呕吐,失眠,荨麻疹、血管神经性水肿和风疹,疲劳,直立性症状,紧张和焦躁,脱发,皮疹,厌食和全身不适,体重增加,头痛,乏力,戒断综合征,短暂肝功能异常。 少见:肌肉关节痛,心悸、心动过速、心动过缓,下肢痉挛,排尿困难,男性乳房发育,尿潴留,更少见有多梦、夜游症、烦躁不安、兴奋、幻视幻听、谵妄、雷诺现象、心力衰竭,心电图异常如传导紊乱、心律失常、乙醇过敏、发烧、短暂血糖升高、血清肌酸磷酸激酶升高、肝炎和腮腺炎等。
- 毒性分级:高毒
- 刺激数据:皮肤-兔 500 毫克 轻度
- 上游原料:2,6-二氯苯胺 --> 氯化氢乙醇溶液 --> 可乐定盐酸盐
- 用法用量:1.降低血压口服,起始剂量0.1 mg,一日2次;需要时隔2~4天递增,每日0.1~0.2mg。常用维持剂量为0.3~0.9mg/日,分2~4次口服。严重高血压需紧急治疗时开始口服0.2mg,继以每小时0.1mg,直到舒张压控制或总量达 0.7mg,然后用维持剂量。 2.绝经期潮热一次0.025~0.075mg,每日2次。 3.严重痛经口服 0.025mg,每日2次,在月经前及月经时,共服14日。 4.偏头痛一次 0.025mg,每日2~4次,最多为 0.05mg,每日3次。 5.极量一次0.6mg,一日2.4mg。
- MOL 文件:4205-90-7.mol
- 用途一:中枢性降压药,用于治疗中度高血压症。
- 注意事项:与噻嗪类利尿剂合用,可增加降压效果,消除水钠潴留,并可减少耐药性及用药剂量。 突然停药可致暂时性交感神经活动亢进。 与三环类抗抑郁药、非类固醇消炎药及β受体阻滞剂并用,盐酸可乐定作用减弱。
- 储运特性:库房通风低温干燥; 轻装轻卸、与氧化剂和酸类分开存放