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'''BRL-50481''' is a drug developed by ] which is the first compound that acts as a ] selective for the PDE<sub>7</sub> subtype.<ref>Smith SJ, Cieslinski LB, Newton R, Donnelly LE, Fenwick PS, Nicholson AG, Barnes PJ, Barnette MS, Giembycz MA. Discovery of BRL 50481 , 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</ref> It has been shown to increase mineralisation activity in ]s, suggesting a potential role for PDE<sub>7</sub> inhibitors in the treatment of ].<ref>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</ref> '''BRL-50481''' is a drug developed by ] which is the first compound that acts as a ] selective for the PDE<sub>7</sub> subtype.<ref>Smith SJ, Cieslinski LB, Newton R, Donnelly LE, Fenwick PS, Nicholson AG, Barnes PJ, Barnette MS, Giembycz MA. Discovery of BRL 50481 , 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</ref> It has been shown to increase mineralisation activity in ]s, suggesting a potential role for ]s in the treatment of ].<ref>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</ref>




Revision as of 09:59, 2 February 2011

Pharmaceutical compound
BRL-50481
Identifiers
IUPAC name
  • N,N,2-Trimethyl-5-nitro-benzenesulfonamide
CAS Number
PubChem CID
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC9H12N2O4S
Molar mass244.267 g/mol g·mol
3D model (JSmol)
SMILES
  • Cc1ccc(N(=O)=O)cc1S(=O)(=O)N(C)C

BRL-50481 is a drug developed by GlaxoSmithKline which is the first compound that acts as a phosphodiesterase inhibitor selective for the PDE7 subtype. It has been shown to increase mineralisation activity in osteoblasts, suggesting a potential role for PDE7 inhibitors in the treatment of osteoporosis.


References

  1. Smith SJ, Cieslinski LB, Newton R, Donnelly LE, Fenwick PS, Nicholson AG, Barnes PJ, Barnette MS, Giembycz MA. Discovery of BRL 50481 , 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
Phosphodiesterase inhibitors
PDE1
PDE2
PDE3
PDE4
PDE5
PDE7
PDE9
PDE10
PDE11BC11-38
Non-selective
Unsorted
See also: Receptor/signaling modulators
Categories: