Moclobemide (Ro 111163)
For research use only.
CAS No. 71320-77-9
Moclobemide is a MAO-A (5-HT) inhibitor with IC50 of 6.1 μM.
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Inguinal adipose stromal cells were differentiated into adipocytes, treated with various chemical inhibitors (1 μM) with or without harmine (1 μM) for 24 h, and then harvested for qPCR and western blot analysis (n = 6 wells/group). Quantitative PCR analysis of Ucp1 expression in the adipocytes treated with harmine and (a) DYRK1A inhibitor, (b) MAO-A inhibitor. Data represent mean ± SEM. *p < 0.05.
Sci Rep, 2016, 6: 36382.. Moclobemide (Ro 111163) purchased from Selleck.
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|Description||Moclobemide is a MAO-A (5-HT) inhibitor with IC50 of 6.1 μM.|
Moclobemide orally administered 2 hours before decapitation preferentially inhibits MAO-A and PEA in rat brain with ED50 of 7.6 μmol/kg and 78 μmol/kg, respectively. Moclobemide orally administered 2 hours before decapitation preferentially inhibits MAO-A and PEA in rat liver with ED50 of 8.4 μmol/kg and 6.6 μmol/kg, respectively. Moclobemide (0.1 mM), which inhibits brain MAO-A activity by over 80%, does not affect benzylamine oxidase (rat heart) and diamine oxidase (rat small intestine) activity in vitro.  Moclobemide (10 mM-100 mM) includes in the culture medium during anoxia or with glutamate significantly increases in a concentration-dependent manner the amount of surviving neurons compared to controls in neuronal-astroglial cultures from rat cerebral cortex. 
|In vivo||Moclobemide (10 mg/kg p.o.) induces a significant decrease of all monoamine metabolites measured in rat brain.  Moclobemide, given via the drinking water (4.5 mg/kg/day), produces significant decreases in adrenal weight of rats after 5 (-23%) and 7 weeks (-16%) of treatment. Moclobemide upregulates hippocampal mineralocorticoid receptor (MR) levels in rats by 65%, 76% and 19% at 2 weeks, 5 weeks and 7 weeks of treatment, and upregulates Glucocorticoid receptor (GR) levels in this limbic brain structure by 10% at 5 weeks. Moclobemide treatment (5 weeks, 4.5 mg/kg/day) significantly attenuates stress (30 min novel environment)-induced plasma ACTH (-35%) and corticosterone (-29%) levels.  Moclobemide (2.5 mg/kg/day) decreases immobility and increases climbing behavior following treatment for 3 days, but increases in both swimming and climbing behaviors are measured following treatment for 14 days. Moclobemide (15 mg/kg/day) decreased immobility and increased swimming for 3 days, whereas treatment for 14 days significantly increases both active behavior (swimming and climbing).  Moclobemide (100 mg/kg/day) combined with triethyltin blocks the development of brain edema and the increase in the cerebral chloride content induced by triethyltin in rats. Moclobemide (100 mg/kg/day) reduces the increase in the cerebral sodium content and attenuates the neurological deficit in rats. |
-  Da Prada M, et al. J Pharmacol Exp Ther, 1989, 248(1), 400-414.
-  Verleye M, et al. Brain Res, 2007, 1138, 30-38.
-  Reul JM, et al. Neuroendocrinology, 1994, 60(5), 509-519.
|In vitro||DMSO||53 mg/mL (197.21 mM)|
|Ethanol||10 mg/mL (37.21 mM)|
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Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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