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司替巴脒

司替巴脒用途

Stilbamidine 是 Stilbene 衍生的二脒化合物,主要以其羟乙基磺酸盐形式发挥作用,用于治疗各种真菌感染。

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司替巴脒名称

[ CAS 号 ]:
122-06-5

[ 中文名 ]:
司替巴脒

[ 英文名 ]:
Stilbamidine

[英文别名 ]:

Stilbamidin
Benzenecarboximidamide,4,4'-(1,2-ethenediyl)bis
4,4'-Vinylenedi(benzamidine)
stilbamidine
trans-stilbene-4,4'-dicarboxamidine
trans-Stilben-4,4'-dicarbamidin
trans-Stilben-dicarbamidin-(4.4')
4,4'-Stilbenedicarboxamidine(7CI,8CI)

司替巴脒生物活性

[ 描述 ]:

Stilbamidine 是 Stilbene 衍生的二脒化合物,主要以其羟乙基磺酸盐形式发挥作用,用于治疗各种真菌感染。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 真菌

研究领域 >> 感染

研究领域 >> 癌症

[ 靶点 ]

fungal

[体外研究]

高亲和性喷他脒转运蛋白(HAPT1)被Propamidine抑制,但对Stilbamidine仅表现出低亲和力。相反,腺苷敏感的喷他脒转运蛋白(ASPT1)被Stilbamidine和Propamidine强烈抑制。 [3H]喷他脒摄取是在各种浓度的腺苷(IC50 =1.2μM)或氧化melarsen(IC50 =0.7μM)存在下,以及在250μM腺苷和浓度升高的次黄嘌呤,丙胺脒(IC50)存在下测定的。 =6.1μM)和Stilbamidine(IC50 =110μM)[1]。两种二脒化合物,Stilbamidine和Pentamidine用于治疗多发性骨髓瘤,这是一种常常发生血清中球蛋白含量增加的疾病[2]。

[参考文献]

[1]. De Koning HP. Uptake of pentamidine in Trypanosoma brucei brucei is mediated by three distinct transporters: implications for cross-resistance with arsenicals. Mol Pharmacol. 2001 Mar;59(3):586-92.

[2]. BREWER AE.et al. Multiple myeloma treated with stilbamidine and pentamidine. Br Med J. 1948 Dec 4;2(4587):978-82.

[相关活性小分子]

司替巴脒物理化学性质

[ 密度 ]:
1.19g/cm3

[ 沸点 ]:
456.4ºC at 760mmHg

[ 分子式 ]:
C₁₆H₁₆N₄

[ 分子量 ]:
264.32500

[ 闪点 ]:
229.8ºC

[ 精确质量 ]:
264.13700

[ PSA ]:
99.74000

[ LogP ]:
4.02520

[ 蒸汽压 ]:
1.62E-08mmHg at 25°C

[ 折射率 ]:
1.634

[ 储存条件 ]:
2-8℃

司替巴脒毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: WJ5250000

CHEMICAL NAME :: 4,4'-Stilbenedicarboxamidine

CAS REGISTRY NUMBER :: 122-06-5

BEILSTEIN REFERENCE NO. :: 3206434

LAST UPDATED :: 199612

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C16-H16-N4

MOLECULAR WEIGHT :: 264.36

WISWESSER LINE NOTATION :: MUYZR D1U1R DYZUM

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 39 mg/kg/29D

TOXIC EFFECTS :: Behavioral - hallucinations, distorted perceptions Lungs, Thorax, or Respiration - respiratory depression Gastrointestinal - nausea or vomiting

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 43 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 115 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 125 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 30 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - hamster

DOSE/DURATION :: 150 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

MUTATION DATA

TYPE OF TEST :: Mutation in microorganisms

TEST SYSTEM :: Yeast - Saccharomyces cerevisiae

DOSE/DURATION :: 190 umol/L

REFERENCE :: EJCODS European Journal of Cancer and Clinical Oncology. (Pergamon Press, c/o Elsevier Science, 660 White Plains Rd., Tarrytown, NY 10591) V.17(7)- 25, 1981-89. For publisher information, see EJCAEL Volume(issue)/page/year: 19,1575,1983

司替巴脒

司替巴脒用途

司替巴脒名称

司替巴脒生物活性

司替巴脒物理化学性质

司替巴脒毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

司替巴脒合成路线

详细合成路线

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