55-65-2

• 常用中文名：依斯美林
• 常用英文名：guanethidine
• CAS号：55-65-2
• 分子式：C₁₀H₂₂N₄
• 分子量：198.30800
• 相关类别： 原料药 循环系统用药 抗高血压病药
• 发布时间：2018-05-18 08:00:00
• 更新时间：2024-01-06 00:27:21
• 硫酸胍于1959年合成。胍被认为通过干扰神经节后交感神经纤维中化学递质的代谢来降低血压。

名称

• 中文名: 依斯美林
• 英文名: guanethidine
• 中文别名: 胍乙啶
• 英文别名: Guanethidinum; Octadine; GUANETHIDINE; (2-<Octahydroazocinyl-(1)>-ethyl)-guanidin; Oktadin; [2-(hexahydro-1-(2H)-azocinyl)ethyl]guanidine; Isobarin; Sanotensin; 2-[2-(azocan-1-yl)ethyl]guanidine; Oktatenzin; (2-azocan-1-yl-ethyl)-guanidine; Ismelin; Eutensol; guanethedine; Abapresin

物化性质

• 密度: 1.13g/cm3
• 沸点: 345.6ºC at 760mmHg
• 分子式: C₁₀H₂₂N₄
• 分子量: 198.30800
• 闪点: 162.8ºC
• 精确质量: 198.18400
• PSA: 65.14000
• LogP: 1.86440
• 折射率: 1.4910 (estimate)

生物活性

• 描述: 硫酸胍于1959年合成。胍被认为通过干扰神经节后交感神经纤维中化学递质的代谢来降低血压。
• 体外研究: 交感神经纤维的消融与大鼠内皮细胞标记物(RECA)的丢失有关,但未发现胍对内皮细胞和间充质干细胞的体外存活有显著影响[1]。
• 体内研究: 胍(30 mg/kg,皮下注射,1小时)作为交感神经阻滞剂在TNFR1(-/-)小鼠中未受影响的IL-18过度伤害[2]。动物模型：野生型(WT)Balb/c、TNFR1(-/-)和IFN-γ-γ(-/-)小鼠[2]。剂量：30mg/kg给药：胍(30mg/kg,皮下注射,1h,在生理盐水中稀释)结果：用胍(交感神经阻滞剂)预处理对TNFR1(-/-)小鼠的IL-18超伤害感受性没有影响。
• 参考文献:

  [1]. P Dubový, etal. Local chemical sympathectomy of rat bone marrow and its effect on marrow cell composition.

  [2]. Waldiceu A.VerriJr, etal. Antigen-induced inflammatory mechanical hypernociception in mice is mediated by IL-18. Brain Beha

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : MF2975000 CHEMICAL NAME : Guanidine, (2-(hexahydro-1(2H)-azocinyl)ethyl)- CAS REGISTRY NUMBER : 55-65-2 LAST UPDATED : 199606 DATA ITEMS CITED : 7 MOLECULAR FORMULA : C10-H22-N4 MOLECULAR WEIGHT : 198.36 WISWESSER LINE NOTATION : T8NTJ A2MYZUM 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 : 1050 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: 26,1671,1976 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 845 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: #3856778 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 100 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value 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: 4,185,1979 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 224 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: #3856778 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 28 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : PCJOAU Pharmaceutical Chemistry Journal (English Translation). Translation of KHFZAN. (Plenum Pub. Corp., 233 Spring St., New York, NY 10013) No.1- 1967- Volume(issue)/page/year: 15,349,1981 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - cat DOSE/DURATION : 50 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 27ZIAQ "Drug Dosages in Laboratory Animals - A Handbook," Rev. ed., Barnes, C.D., and L.G. Eltherington, Berkeley, Univ. of California Press, 1973 Volume(issue)/page/year: -,112,1973 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 50 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 27ZIAQ "Drug Dosages in Laboratory Animals - A Handbook," Rev. ed., Barnes, C.D., and L.G. Eltherington, Berkeley, Univ. of California Press, 1973 Volume(issue)/page/year: -,112,1973

合成路线

1126-67-6 1184-90-3 ~% 55-65-2

文献：US4656291 A1, ;

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