BRL-50481
Chemical compound
- None
- N,N,2-Trimethyl-5-nitrobenzenesulfonamide
- 433695-36-4 Y
- 2921148
- 5154
- 2194720 N
- 03G869PR3P
- CHEBI:93472
- ChEMBL484928 N
- DTXSID30195832
- Interactive image
- Cc1ccc(N(=O)=O)cc1S(=O)(=O)N(C)C
InChI
- InChI=1S/C9H12N2O4S/c1-7-4-5-8(11(12)13)6-9(7)16(14,15)10(2)3/h4-6H,1-3H3 N
- Key:IFIUFCJFLGCQPH-UHFFFAOYSA-N N
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]
References
- ^ 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. PMID 15371556. S2CID 9491524.
- ^ 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. PMC 2854023. PMID 20228279.
- ^ 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.
- v
- t
- e
- BAY 60-7550
- Carbazeran
- EHNA
- Oxindole
- PDP
- Adibendan
- Amrinone (inamrinone)
- Anagrelide
- Benafentrine
- Bucladesine
- Carbazeran
- Cilostamide
- Cilostazol
- Enoximone
- Imazodan
- KMUP-1
- Meribendan
- Milrinone
- Olprinone
- Parogrelil
- Pimobendan
- Pumafentrine
- Quazinone
- RPL-554
- Siguazodan
- Trequinsin
- Vesnarinone
- Zardaverine
- Apremilast
- Arofylline
- Atizoram
- Benafentrine
- Catramilast
- CC-1088
- CDP-840
- CGH-2466
- Cilomilast
- Cipamfylline
- Crisaborole
- Denbutylline
- Difamilast
- Drotaverine
- Etazolate
- Filaminast
- Glaucine
- HT-0712
- ICI-63197
- Indimilast
- Irsogladine
- Lavamilast
- Lirimilast
- Lotamilast
- Luteolin
- Mesembrenone
- Mesembrine
- Mesopram
- Oglemilast
- Piclamilast
- Pumafentrine
- Revamilast
- Ro 20-1724
- Roflumilast
- Rolipram
- Ronomilast
- RPL-554
- RS-25344
- Tetomilast
- Tofimilast
- YM-976
- Zardaverine
- Acetildenafil
- Aildenafil
- Avanafil
- Beminafil
- Benzamidenafil
- Dasantafil
- Icariin
- Gisadenafil
- Homosildenafil
- Lodenafil
- Mirodenafil
- MY-5445
- Nitrosoprodenafil
- Norcarbodenafil
- SCH-51866
- Sildenafil
- Sulfoaildenafil
- T-0156
- Tadalafil
- Udenafil
- Vardenafil
- BRL-50481
- BAY 73-6691
- PF-04447943
- Paraxanthine
- Balipodect
- Mardepodect
- Papaverine
- TC-E 5005
- Tofisopam
BC11-38
- Diazepam
- Diprophylline
- DPCPX
- Furafylline
- Lisofylline
- MDL-12330A
- Moxaverine
- Oxagrelate
- Pentifylline
- Proxyphylline
- Quercetin
- Satigrel
- Tolafentrine
- Trapidil
See also: Receptor/signaling modulators