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Chemical Compound Review

Tebufelona     1-(4-hydroxy-3,5-ditert- butyl-phenyl)hex-5...

Synonyms: Tebufelone, Tebufelonum, CHEMBL13878, CHEBI:113173, NE-11740, ...
 
 
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Disease relevance of NE 11740

 

High impact information on NE 11740

  • The addition of the CO/5-LO inhibitor 2 h after LPS stimulation, however, did not interfere with IL 1 beta synthesis, suggesting that tebufelone interacts with an early event(s) in the activation of PBMC [2].
  • We examined the effect of tebufelone, a dual cyclooxygenase (CO)/5-lipoxygenase (LO) inhibitor, on the synthesis, secretion and gene expression of interleukin (IL) 1 beta and tumor necrosis factor (TNF)-alpha by human peripheral blood mononuclear cells (PBMC) [2].
  • Transcription, translation and secretion of interleukin 1 and tumor necrosis factor: effects of tebufelone, a dual cyclooxygenase/5-lipoxygenase inhibitor [2].
  • In conclusion, we have demonstrated that tebufelone enhances IL 1 (alpha and beta) and TNF-alpha synthesis at concentrations which suppress leukotriene formation [2].
  • The greatest increase in CYP2B11 markers produced by tebufelone treatment ranged from 2- to 3-fold, whereas the increase in CYP3A12 markers ranged from 5- to 10-fold [1].
 

Biological context of NE 11740

 

Anatomical context of NE 11740

  • Comparison of tebufelone distribution in rat blood plasma and inflamed and noninflamed tissues following peroral and intravenous administration [5].
  • Electron microscopic evaluation, however, revealed marked dose-dependent increases in smooth endoplasmic reticulum in all of the tebufelone treatment groups [1].
  • The purpose of the present study was to assess the effects of tebufelone on hepatocyte ultrastructure and hepatic cytochromes p450 (P450s) in the beagle dog after 2 weeks of oral administration at dose levels of 0, 5, 15, 50, and 100 mg/kg/day (N = 1/sex/dose level) [1].
 

Associations of NE 11740 with other chemical compounds

 

Gene context of NE 11740

 

Analytical, diagnostic and therapeutic context of NE 11740

References

  1. Characterization of the effects of tebufelone on hepatic cytochromes P450 in the beagle dog. Smith, B.J., Zupan, L.A., Hu, J.K., Diters, R.W., Gibson, G.W., Norton, J.N. Drug Metab. Dispos. (1996) [Pubmed]
  2. Transcription, translation and secretion of interleukin 1 and tumor necrosis factor: effects of tebufelone, a dual cyclooxygenase/5-lipoxygenase inhibitor. Sirko, S.P., Schindler, R., Doyle, M.J., Weisman, S.M., Dinarello, C.A. Eur. J. Immunol. (1991) [Pubmed]
  3. Absorption, bioavailability, and pharmacokinetics of tebufelone in the rat. Sietsema, W.K., Kelm, G.R., Deibel, R.M., Doyle, M.J., Loomans, M.E., Smyth, R.E., Kinnett, G.O., Eichhold, T.H., Farmer, R.W. Journal of pharmaceutical sciences. (1993) [Pubmed]
  4. Interspecies scaling of tebufelone pharmacokinetic data and application to preclinical toxicology. Cruze, C.A., Kelm, G.R., Meredith, M.P. Pharm. Res. (1995) [Pubmed]
  5. Comparison of tebufelone distribution in rat blood plasma and inflamed and noninflamed tissues following peroral and intravenous administration. Doyle, M.J., Eichhold, T.H., Loomans, M.E., Farmer, R.W., Kelm, G.R. Journal of pharmaceutical sciences. (1993) [Pubmed]
  6. Determination of leukotriene B4 in human plasma by gas chromatography using a mass selective detector and a stable isotope labelled internal standard. Effect of NE-11740 on arachidonic acid metabolism. Doyle, M.J., Eichhold, T.H., Hynd, B.A., Weisman, S.M. Journal of pharmaceutical and biomedical analysis. (1990) [Pubmed]
  7. Long-term performance of a gas chromatography/tandem mass spectrometry assay for tebufelone in plasma. Dobson, R.L., Neal, D.M., DeMark, B.R., Ward, S.R. Anal. Chem. (1990) [Pubmed]
  8. Determination of tebufelone (a new anti-inflammatory drug) strength and stability in bulk drug, dosage formulations and feed admixtures by reversed-phase high-performance liquid chromatography. Kaffenberger, R.M., Eichhold, T.H., Doyle, M.J. J. Chromatogr. (1990) [Pubmed]
 
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