4,4′-STILBENEDICARBOXAMIDINE, DIHYDROCHLORIDE

Stilbamidine dihydrochloride is a diamidine compound derived from Stilbene and used chiefly in the form of its crystalline isethionate salt in treating various fungal infections.

Research Areas >> Cancer

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Fungal

高亲和力 pentamidine 转运蛋白 (HAPT1) 被 Propamidine 抑制，但对 Stilbamidine dihydrochloride 仅显示低亲和力。相反，腺苷敏感的 pentamidine 转运蛋白 (ASPT1) 会被二盐酸二苯巴脒和 Propamidine 强烈抑制。在不同浓度的腺苷 (IC50=1.2 μM) 或 Melarsen oxide (IC50=0.7 μM) 存在下测定 [3H]pentamidine 摄取=0.7 μM)，以及存在 250 μM 腺苷和增加浓度的次黄嘌呤、Propamidine (IC50=6.1 μM) 和 Stilbamidine dihydrochloride (IC50=110 μM)[1]。两种二脒化合物，Stilbamidine dihydrochloride 和 Pentamidine 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]。

[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.  

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