依斯美林

依斯美林用途

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。

依斯美林名称

[ CAS 号 ]:
55-65-2

[ 中文名 ]:
依斯美林

[ 英文名 ]:
guanethidine

[中文别名 ]:

[英文别名 ]:

依斯美林生物活性

[ 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

依斯美林物理化学性质

[ 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)

依斯美林毒性和生态

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

依斯美林合成路线

详细合成路线

依斯美林上下游产品

依斯美林上游产品

依斯美林下游产品

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