136959-96-1
Chemical Structure
RU 43044
- CAS No.: 136959-96-1
- Formula:C29H34O2
- Molecular Weight:414.58
IUPAC Name: (8S,10R,13S,14S,17S)-17-hydroxy-13-methyl-10-(4-methylbenzyl)-17-(prop-1-yn-1-yl)-1,2,6,7,8,10,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one
InChIKey: NSUUUQRFPXZFLI-ZPCMSWJYSA-N
SMILES: O=C1CC[C@@]2(C3=CC[C@@]4([C@@](O)(CC[C@]4([C@@]3(CCC2=C1)[H])[H])C#CC)C)CC5=CC=C(C=C5)C
Biological Activity: RU 43044 is an orally active, selective glucocorticoid receptor inhibitor. RU 43044 blocks glucocorticoid receptor activity and reverses the enhanced dopamine release induced by high potassium in the prefrontal cortex. RU 43044 also inhibits thymocyte receptor down-regulation induced by high-dose glucocorticoids without affecting thymocyte apoptosis or basal receptor expression. RU 43044 is widely applicable to research related to depression[1][2][3].
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RU 43044 | RU 43044 is an orally active, selective glucocorticoid receptor inhibitor. RU 43044 blocks glucocorticoid receptor activity and reverses the enhanced dopamine release induced by high potassium in the prefrontal cortex. RU 43044 also inhibits thymocyte receptor down-regulation induced by high-dose glucocorticoids without affecting thymocyte apoptosis or basal receptor expression. RU 43044 is widely applicable to research related to depression. | |||||||||||||||||||||
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- [1]. Ago Y, et al. Antidepressant-like effects of the glucocorticoid receptor antagonist RU-43044 are associated with changes in prefrontal dopamine in mouse models of depression. Neuropharmacology. 2008;55(8):1355-1363. [Content Brief]
- [2]. Clark R D, et al. 2-Benzenesulfonyl-8a-benzyl-hexahydro-2H-isoquinolin-6-ones as selective glucocorticoid receptor antagonists[J]. Bioorganic & medicinal chemistry letters, 2007, 17(20): 5704-5708.
- [3]. Berki T, et al. Glucocorticoid (GC) sensitivity and GC receptor expression differ in thymocyte subpopulations. Int Immunol. 2002;14(5):463-469. [Content Brief]
Keywords
