BRL-50481
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| Formula | C9H12N2O4S |
| Molar mass | 244.27g·mol−1 |
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BRL-50481is a drug developed byGlaxoSmithKlinewhich is the first compound that acts as aphosphodiesterase inhibitorselective for thePDE7family.[1]PDE7 activity is encoded by two genes,PDE7AandPDE7B.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 inosteoblasts,suggesting a potential role forPDE7 inhibitorsin the treatment ofosteoporosis.[3]
References
[edit]- ^Smith SJ, Cieslinski LB, Newton R, Donnelly LE, Fenwick PS, Nicholson AG, et al. (December 2004)."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"(PDF).Molecular Pharmacology.66(6): 1679–89.doi:10.1124/mol.104.002246.PMID15371556.S2CID9491524.
- ^Alaamery MA, Wyman AR, Ivey FD, Allain C, Demirbas D, Wang L, et al. (April 2010)."New classes of PDE7 inhibitors identified by a fission yeast-based HTS".Journal of Biomolecular Screening.15(4): 359–67.doi:10.1177/1087057110362100.PMC2854023.PMID20228279.
- ^Pekkinen M, Ahlström ME, Riehle U, Huttunen MM, Lamberg-Allardt CJ (July 2008). "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.doi:10.1016/j.bone.2008.02.021.PMID18420479.