Discovery of BRL 50481 [3-(N,N-dimethylsulfonamido)-4-methyl-nitrobenzene], a selective inhibitor of phosphodiesterase 7: in vitro studies in human monocytes, lung macrophages, and CD8+ T-lymphocytes.

@article{Smith2004DiscoveryOB,
  title={Discovery of BRL 50481 [3-(N,N-dimethylsulfonamido)-4-methyl-nitrobenzene], a selective inhibitor of phosphodiesterase 7: in vitro studies in human monocytes, lung macrophages, and CD8+ T-lymphocytes.},
  author={Susan J. Smith and Lenora B. Cieslinski and Robert Newton and Louise E Donnelly and Peter S. Fenwick and Andrew G. Nicholson and Peter J Barnes and Mary S. Barnette and Mark A. Giembycz},
  journal={Molecular pharmacology},
  year={2004},
  volume={66 6},
  pages={
          1679-89
        }
}
The biochemical and pharmacological characteristics in human proinflammatory cells of BRL 50481 [3-(N,N-dimethylsulfonamido)-4-methyl-nitrobenzene], a novel and selective inhibitor of phosphodiesterase (PDE) 7, are described. BRL 50481 inhibited the activity of hrPDE7A1 expressed in baculovirus-infected Spodoptera frugiperda 9 cells in a competitive manner (Ki value of 180 nM) and was 416 and 1884 times less potent against PDE3 and 38 and 238 times less potent against PDE4 at a substrate… CONTINUE READING

Citations

Publications citing this paper.
SHOWING 1-10 OF 57 CITATIONS, ESTIMATED 39% COVERAGE

PDE7A1 hydrolyzes cCMP.

VIEW 12 EXCERPTS
CITES BACKGROUND & METHODS
HIGHLY INFLUENCED

Cloning, stable expression of human phosphodiesterase 7A and development of an assay for screening of PDE7 selective inhibitors

  • Applied Microbiology and Biotechnology
  • 2007
VIEW 5 EXCERPTS
CITES BACKGROUND, METHODS & RESULTS
HIGHLY INFLUENCED

Different mitogen-activated protein kinase-dependent cytokine responses in cells of the monocyte lineage.

  • The Journal of pharmacology and experimental therapeutics
  • 2007
VIEW 7 EXCERPTS
CITES METHODS & BACKGROUND
HIGHLY INFLUENCED

PDE4 inhibitors as potential therapeutic agents in the treatment of COPD-focus on roflumilast

  • International journal of chronic obstructive pulmonary disease
  • 2007
VIEW 4 EXCERPTS
CITES BACKGROUND
HIGHLY INFLUENCED

PDE4 inhibitors: current status.

  • British journal of pharmacology
  • 2008
VIEW 5 EXCERPTS
CITES BACKGROUND
HIGHLY INFLUENCED

Epac Function and cAMP Scaffolds in the Heart and Lung

  • Journal of cardiovascular development and disease
  • 2018
VIEW 1 EXCERPT
CITES BACKGROUND

FILTER CITATIONS BY YEAR

2005
2019

CITATION STATISTICS

  • 8 Highly Influenced Citations

References

Publications referenced by this paper.
SHOWING 1-10 OF 51 REFERENCES

Ubiquitous expression of phosphodiesterase 7A in human proinflammatory and immune cells.

  • American journal of physiology. Lung cellular and molecular physiology
  • 2003
VIEW 12 EXCERPTS
HIGHLY INFLUENTIAL

Phosphodiesterase 7A-deficient mice have functional T cells.

  • Journal of immunology
  • 2003
VIEW 3 EXCERPTS
HIGHLY INFLUENTIAL

Development status of second generation PDE4 inhibitors for asthma and COPD: the story so far.

  • Monaldi archives for chest disease = Archivio Monaldi per le malattie del torace
  • 2002
VIEW 6 EXCERPTS
HIGHLY INFLUENTIAL

T cell activation up-regulates cyclic nucleotide phosphodiesterases 8A1 and 7A3.

  • Proceedings of the National Academy of Sciences of the United States of America
  • 2001
VIEW 6 EXCERPTS
HIGHLY INFLUENTIAL

Similar Papers

Loading similar papers…