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A novel dual regulator of tumor necrosis factor-alpha and interleukin-10 protects mice from endotoxin-induced shock.

Abstract
A pyrimidylpiperazine derivative, N-[1-(4-¿[4-(pyrimidin-2-yl)piperazin-1-yl]methyl¿phenyl)cycloprop yl] acetamide (Y-39041), is a dual cytokine regulator of tumor necrosis factor (TNF)-alpha and interleukin-10 production. Lipopolysaccharide-induced TNF-alpha release in BALB/c mice was inhibited by the oral treatment with the compound at 10-100 mg/kg (about 80% suppression) while interleukin-10 release was augmented (about 10-fold increase at 30 mg/kg). In addition, Y-39041 (30 mg/kg, p.o.) completely protected mice from lipopolysaccharide-induced death by the treatment before and after lipopolysaccharide injection. The finding that Y-39041 suppresses TNF-alpha production and stimulates interleukin-10 production at the same time provides new insights for the treatment of septic shock, rheumatoid arthritis and Crohn's diseases.
AuthorsT Fukuda, H Sumichika, M Murata, T Hanano, K Adachi, M Hisadome
JournalEuropean journal of pharmacology (Eur J Pharmacol) Vol. 391 Issue 3 Pg. 317-20 (Mar 17 2000) ISSN: 0014-2999 [Print] Netherlands
PMID10729374 (Publication Type: Journal Article)
Chemical References
  • Acetamides
  • Endotoxins
  • Lipopolysaccharides
  • Piperazines
  • Tumor Necrosis Factor-alpha
  • Y 39041
  • Interleukin-10
  • endotoxin, Escherichia coli
Topics
  • Acetamides (administration & dosage, pharmacology)
  • Administration, Oral
  • Animals
  • Endotoxins
  • Enzyme-Linked Immunosorbent Assay
  • Escherichia coli
  • Female
  • Interleukin-10 (biosynthesis)
  • Lipopolysaccharides
  • Mice
  • Mice, Inbred BALB C
  • Piperazines (administration & dosage, pharmacology)
  • Shock, Septic (chemically induced, metabolism, mortality, prevention & control)
  • Tumor Necrosis Factor-alpha (biosynthesis)

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