Synonyms: BOL-303242-X | ZK-245186 | ZK245186
Compound class:
Synthetic organic
Comment: Mapracorat is a novel non-steroidal selective glucocorticoid receptor agonist (SEGRA) [3-4]. SEGRAs exert their pharmacological effect by activating only the transrepression pathway, which is in contrast to traditional glucocorticosteroids (GCs) which activate both the transactivation and transrepression pathways.The pharmaceutical industry is trying to develop new GCs that are as effective as traditional GCs, but with fewer limiting adverse effects. Mapracorat and GSK866 are prototype compounds that were designed to address this clinical need.
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References |
1. Baiula M, Bedini A, Baldi J, Cavet ME, Govoni P, Spampinato S. (2014)
Mapracorat, a selective glucocorticoid receptor agonist, causes apoptosis of eosinophils infiltrating the conjunctiva in late-phase experimental ocular allergy. Drug Des Devel Ther, 8: 745-57. [PMID:24959069] |
2. Baiula M, Spampinato S. (2014)
Mapracorat, a novel non-steroidal selective glucocorticoid receptor agonist for the treatment of allergic conjunctivitis. Inflamm Allergy Drug Targets, 13 (5): 289-98. [PMID:25373600] |
3. Schäcke H, Zollner TM, Döcke WD, Rehwinkel H, Jaroch S, Skuballa W, Neuhaus R, May E, Zügel U, Asadullah K. (2009)
Characterization of ZK 245186, a novel, selective glucocorticoid receptor agonist for the topical treatment of inflammatory skin diseases. Br J Pharmacol, 158 (4): 1088-103. [PMID:19422381] |
4. Zhang JZ, Cavet ME, VanderMeid KR, Salvador-Silva M, López FJ, Ward KW. (2009)
BOL-303242-X, a novel selective glucocorticoid receptor agonist, with full anti-inflammatory properties in human ocular cells. Mol Vis, 15: 2606-16. [PMID:20011631] |