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={S. J. Smith and L. Cieslinski and R. Newton and L. Donnelly and P. Fenwick and A. Nicholson and P. Barnes and M. Barnette and M. Giembycz},
  journal={Molecular Pharmacology},
  year={2004},
  volume={66},
  pages={1679 - 1689}
}
  • S. J. Smith, L. Cieslinski, +6 authors M. Giembycz
  • Published 2004
  • Biology, Medicine
  • Molecular Pharmacology
  • 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
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