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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- CAS No.: 136959-96-1
- Formule: C29H34O2
- Masse moléculaire:414.58
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
RU 43044 (10-30 mg/kg; p.o.; administered at 23.5, 5, and 1 hours before experiments) produces antidepressant-like effects in isolation-reared mice, reversing increased forced swim test immobility and enhanced prefrontal high K+-stimulated dopamine release, without altering motor function[1].
RU 43044 (1 mg/kg; i.p.; every 12 hours; 2 days) alone has no effect on normal thymocyte development or GCR expression, but it blocks high-dose Dexamethasone (HY-14648) -induced GCR down-regulation in mature single-positive thymocytes[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ddY mice (male, 5 weeks old at study initiation, chronic corticosterone-induced)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:p.o.; administered at 23.5, 5, and 1 hours before experiments
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Result:Significantly reversed the increased immobility time in the forced swim test caused by chronic corticosterone treatment at 10 mg/kg and 30 mg/kg.
Reversed the chronic corticosterone-induced enhancement of high K+-stimulated dopamine release in the prefrontal cortex at 30 mg/kg.
Did not affect basal dopamine release, basal serotonin release, or high K+-stimulated serotonin release in chronic corticosterone-treated mice at 30 mg/kg.
Had no effect on spontaneous locomotor activity or rotarod performance in chronic corticosterone-treated mice at 30 mg/kg.
Chemical Information
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CAS No. 136959-96-1
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Masse moléculaire 414.58
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Formule C29H34O2
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RU 43044 Related Classifications
HY-120016 Related Classifications
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