6935-63-3

• 常用中文名：司替巴脒二盐酸盐
• 常用英文名：4,4′-STILBENEDICARBOXAMIDINE, DIHYDROCHLORIDE
• CAS号：6935-63-3
• 分子式：C₁₆H₁₈Cl₂N₄
• 分子量：337.25
• 相关类别： 信号通路 抗感染 真菌
• 发布时间：2017-05-07 03:33:24
• 更新时间：2024-04-05 18:14:51
• 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。

名称

• 中文名: 司替巴脒二盐酸盐
• 英文名: trans-stilbene-4,4'-dicarboxamidine, dihydrochloride

物化性质

• 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

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.

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