ORG-34517 is currently under investigation by Organon for the treatment of depression. It has potential to treat a number of diseases such as Cushing’s disease, hypertension, diabetes, glaucoma etc, in which the activity of metabolites corticosterone and cortisol is high.
Org-34517 is a glucocorticoid antagonist which may have a potential in a number of diseases where there is excess corticosterone/cortisol activity. The drug acts by normalizing hyperactivity in the hypothalamus-pituitary-adrenal (HPA) axis.
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Bilang-Bleuel A, Ulbricht S, Chandramohan Y, De Carli S, Droste SK, Reul JM: Psychological stress increases histone H3 phosphorylation in adult dentate gyrus granule neurons: involvement in a glucocorticoid receptor-dependent behavioural response. Eur J Neurosci. 2005 Oct;22(7):1691-700. [PubMed:16197509 ]
Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modulator of other transcription factors. Affects inflammatory responses, cellular proliferation and differentiation in target tissues. Could act as a coactivator for STAT5-dependent transcription upon grow...