BRL-50481

BRL-50481
Systematic (IUPAC) name
N,N,2-Trimethyl-5-nitro-benzenesulfonamide
Clinical data
Identifiers
433695-36-4 Yes
PubChem CID 2921148
ChemSpider 2194720 
ChEMBL CHEMBL484928 
Chemical data
Formula C9H12N2O4S
244.267 g/mol
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BRL-50481 is a drug developed by GlaxoSmithKline which is the first compound that acts as a phosphodiesterase inhibitor selective for the PDE7 subtype.[1] It has been shown to increase mineralisation activity in osteoblasts, suggesting a potential role for PDE7 inhibitors in the treatment of osteoporosis.[2]


References

  1. Smith SJ, Cieslinski LB, Newton R, Donnelly LE, Fenwick PS, Nicholson AG, Barnes PJ, Barnette MS, Giembycz MA. 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. Molecular Pharmacology. 2004 Dec;66(6):1679-89. PMID 15371556
  2. Pekkinen M, Ahlström ME, Riehle U, Huttunen MM, Lamberg-Allardt CJ. Effects of phosphodiesterase 7 inhibition by RNA interference on the gene expression and differentiation of human mesenchymal stem cell-derived osteoblasts. Bone. 2008 Jul;43(1):84-91. PMID 18420479