Benznidazole

Catalog No.S3741 Synonyms: Radanil

For research use only.

Benznidazole (Radanil) is a nitroimidazole derivative having an antiprotozoal activity by interfering with parasite protein biosynthesis, influencing cytokines production and stimulating host phagocytosis.

Benznidazole Chemical Structure

CAS No. 22994-85-0

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Biological Activity

Description Benznidazole (Radanil) is a nitroimidazole derivative having an antiprotozoal activity by interfering with parasite protein biosynthesis, influencing cytokines production and stimulating host phagocytosis.
In vitro

Benznidazole (BZL) inhibits the proliferation of leukemic non-adherent cells by controlling cell cycle at G0/G1 cell phase through up-regulation of p27. Growth inhibition induced by BZL is a reversible process, not accompanied by significant cell death. Besides its trypanocidal activity, BZL also has an immunomodulatory effect on macrophages by blocking the transcription of some pro-inflammatory mediators without altering interleukin 10 expression[1].

In vivo In mice, oral administration of Benznidazole (100 mg/kg): the time to reach maximum concentration (Tmax) in plasma was 0.83 h, and the maximum concentration (Cmax) in plasma was 41.61 μg/ml. The elimination half-life (t1/2b) of Benznidazole was 2.03 h, and mean residence time (MRT) was 3.86 h. The volume of distribution (V) and clearance (CL), both as a function of Benznidazole bioavailability (F), were 38.81 ml and 13.29 ml/h, respectively. In Wistar rats treated orally, Tmaxs of Benznidazole are 2.0 and 1.1 h, respectively. Tmaxs of 15, 30, or 60 min, depending on the dose, in BALB/c mice following intraperitoneal treatment and Tmaxs of 1 to 5 h for dogs treated orally. Benznidazole can cross the blood-brain barrier and exert its action in cases of central nervous system parasitism. However, other studies have indicated that BNZ has toxic effects in the central nervous system. Dogs orally treated with BNZ presented encephalopathy with multifocal characteristics and clinical, pathological, and neurological disorders that were dose dependent and time dependent. Benznidazole biodistribution occurs broadly, reaching the heart and colon, which are the most relevant organs for T. cruzi infection, and also the spleen, brain, liver, lungs, and kidneys[2].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: THP-1 cells
  • Concentrations: 0.1, 0.5 or 1 mM
  • Incubation Time: 24 or 48 h
  • Method:

    20000 cells in 200 mL of complete medium were incubated in quadruplicate in a 96-well plate in the presence of BZL (0.1, 0.5 and 1 mM) or vehicle (0.1% DMSO) for 24 or 48 h and then 20 mL of MTT solution (5 mg/mL in phosphate-buffered saline [PBS]) was added to each well. After 2 h at 37 ℃, the MTT solution was removed and precipitated formazan was solubilized in 200 mL DMSO. Formazan production was then measured at OD545nm in a micro plate spectrophotometer, with DMSO as blank.

Animal Research:

[2]

  • Animal Models: Swiss mice 
  • Dosages: 100 mg/kg
  • Administration: by gavage

Solubility (25°C)

In vitro

DMSO 52 mg/mL
(199.8 mM)
Water Insoluble
Ethanol ''5 mg/mL

Chemical Information

Molecular Weight 260.25
Formula

C12H12N4O3

CAS No. 22994-85-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C=C1)CNC(=O)CN2C=CN=C2[N+](=O)[O-]

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03892213 Completed Drug: Benznidazole|Drug: E1224 Chagas Disease Drugs for Neglected Diseases|PHINC DEVELOPMENT October 2014 Phase 1
NCT01755403 Completed Drug: Benznidazole Chagas Disease Barcelona Centre for International Health Research December 2012 Phase 4
NCT01547533 Completed -- Chagas Disease|Lactation Hospital de Niños R. Gutierrez de Buenos Aires August 2011 --
NCT01489228 Unknown status Drug: E1224|Drug: Benznidazole|Drug: Placebo Chronic Chagas Disease Indeterminate Drugs for Neglected Diseases|Eisai Co. Ltd. June 2011 Phase 2
NCT00699387 Completed Drug: Benznidazole Chagas Disease Hospital de Niños R. Gutierrez de Buenos Aires|Thrasher Research Fund|The Hospital for Sick Children|Fundacion Bunge y Born (Argentina)|Universidad Nacional de La Plata|Consejo de Investigacion en Salud Gobierno de Buenos Aires April 2007 Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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