BRL-50481 explained

BRL-50481 is a drug developed by GlaxoSmithKline which is the first compound that acts as a phosphodiesterase inhibitor selective for the PDE7 family.^[1] PDE7 activity is encoded by two genes, PDE7A and PDE7B. BRL-50481 actually shows about an 80-fold preference for the PDE7A subtype, for which it was developed, over PDE7B.^[2] BRL-50481 has been shown to increase mineralisation activity in osteoblasts, suggesting a potential role for PDE7 inhibitors in the treatment of osteoporosis.^[3]

Notes and References

1. Smith SJ, Cieslinski LB, Newton R, Donnelly LE, Fenwick PS, Nicholson AG, Barnes PJ, Barnette MS, Giembycz MA . 6 . 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 . 66 . 6 . 1679–89 . December 2004 . 15371556 . 10.1124/mol.104.002246 . 9491524 .
2. Alaamery MA, Wyman AR, Ivey FD, Allain C, Demirbas D, Wang L, Ceyhan O, Hoffman CS . 6 . New classes of PDE7 inhibitors identified by a fission yeast-based HTS . Journal of Biomolecular Screening . 15 . 4 . 359–67 . April 2010 . 20228279 . 2854023 . 10.1177/1087057110362100 .
3. 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 . 43 . 1 . 84–91 . July 2008 . 18420479 . 10.1016/j.bone.2008.02.021 .