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司替巴脒二盐酸盐

司替巴脒二盐酸盐用途

二氢二苯胺是二苯乙烯衍生的二苯胺化合物,主要以其结晶异硫氰酸盐的形式用于治疗各种真菌感染。

司替巴脒二盐酸盐名称

[ CAS 号 ]:
6935-63-3

[ 中文名 ]:
司替巴脒二盐酸盐

[ 英文名 ]:
4,4′-STILBENEDICARBOXAMIDINE, DIHYDROCHLORIDE

司替巴脒二盐酸盐生物活性

[ 描述 ]:

二氢二苯胺是二苯乙烯衍生的二苯胺化合物,主要以其结晶异硫氰酸盐的形式用于治疗各种真菌感染。

[ 相关类别 ]:

研究领域 >> 癌症

研究领域 >> 感染

信号通路 >> 抗感染 >> 真菌

[体外研究]

高亲和力五脒转运蛋白 (第1章)被丙脒抑制,但对二氢Stibamidine仅显示低亲和力。相反,腺苷敏感的五脒转运蛋白 (ASPT1)会被二盐酸二苯巴脒和丙脒强烈抑制。在不同浓度的腺苷 (IC50=1.2μM)或氧化三聚氰胺(IC50=0.7μM)存在下测定 [3H]戊脒摄取=0.7μ以及存在 250微米腺苷和增加浓度的次黄嘌呤、丙脒(IC50=6.1μM)和二氢Stilbamidine二盐酸盐(IC50=110μM)[1]两种二脒化合物,二氢Stibamidine和五脒用于治疗多发性骨髓瘤,这种疾病经常发生血清球蛋白含量增加[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.

司替巴脒二盐酸盐物理化学性质

[ 沸点 ]:
456.4ºC at 760 mmHg

[ 分子式 ]:
C₁₆H₁₈Cl₂N₄

[ 分子量 ]:
337.25

[ 闪点 ]:
229.8ºC

[ 精确质量 ]:
300.11400

[ PSA ]:
99.74000

[ LogP ]:
4.82720

司替巴脒二盐酸盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: WJ5340000

CHEMICAL NAME :: 4,4'-Stilbenedicarboxamidine, dihydrochloride

CAS REGISTRY NUMBER :: 6935-63-3

LAST UPDATED :: 199712

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C16-H16-N4.2Cl-H

MOLECULAR WEIGHT :: 337.28

WISWESSER LINE NOTATION :: MUYZR D1U1R DYZUM &GH 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 91 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 2,581,1952

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 180 mg/kg

TOXIC EFFECTS :: Brain and Coverings - recordings from specific areas of CNS Lungs, Thorax, or Respiration - other changes Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: ATMPA2 Annals of Tropical Medicine and Parasitology. (Grune & Stratton, Inc., POB 6280, Duluth, MN 55806) V.1- 1907- Volume(issue)/page/year: 37,1,1943

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 18900 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 2,581,1952 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 360 mg/kg/10D-I

TOXIC EFFECTS :: Vascular - regional or general arteriolar or venous dilation Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: ATMPA2 Annals of Tropical Medicine and Parasitology. (Grune & Stratton, Inc., POB 6280, Duluth, MN 55806) V.1- 1907- Volume(issue)/page/year: 37,1,1943