BRL-50481

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]

BRL-50481
Clinical data
ATC code
  • None
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC9H12N2O4S
Molar mass244.267 g/mol g·mol−1
3D model (JSmol)
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References
  1. Smith, SJ; Cieslinski, LB; Newton, R; Donnelly, LE; Fenwick, PS; Nicholson, AG; Barnes, PJ; Barnette, MS; Giembycz, MA (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. PMID 15371556. Retrieved 5 October 2016.
  2. Alaamery, M.A.; Wyman, A.R.; Ivey. F.D.; Allain, C.; Demirbas, D.; Wang, L.; Ceyhan, O.; Hoffman, C.S. (2010). "New classes of PDE7 inhibitors identified by a fission yeast-based HTS". J. Biomol. Screening. 15: 359–367. doi:10.1177/1087057110362100. PMC 2854023. PMID 20228279.
  3. 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. PMID 18420479.
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