product name Moclobemide (Ro 111163)
Description: Moclobemide is a reversible MAO-A (5-HT) inhibitor with IC50 of 6.1 μM. It is primarily used for the treatment of depression and social anxiety. Moclobemide is a prototype of RIMA agents. It is found to possess antidepressant efficacy with less risk of fatal side-effects like hypertensive crisis. Moclobemide shows a weak but specific inhibition of MAO-A in the in vitro assay using rat brain homogenates.
References: J Pharmacol Exp Ther. 1989 Jan;248(1):400-14; Neuroendocrinology. 1994 Nov;60(5):509-19.
268.74
Formula
C13H17ClN2O2
CAS No.
71320-77-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 53 mg/mL (197.2 mM)
Water: <1 mg/mL
Ethanol: 10 mg/mL (37.2 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: Moclobemide is a prototype of RIMA agents. It is found to possess antidepressant efficacy with less risk of fatal side-effects like hypertensive crisis. Moclobemide shows a weak but specific inhibition of MAO-A in the in vitro assay using rat brain homogenates. The IC50 values of MAO-A and MAO-B in the assay are 6mM and 1000mM, respectively. In ex vivo animal experiments, moclobemide produces an inhibition of 80% in the brain and liver. Additionally, the long-term administration of high doses of moclobemide is found to down-regulate β-adrenoceptors and increase the agonist binding affinity of α1-adrenoceptors. Moreover, moclobemide is rapidly and almost completely absorbed after oral administration. The bioavailability of moclobemide is about 50% after a single administration of 100 mg . |
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| 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. |
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| Formulation & Dosage | |
| References | J Pharmacol Exp Ther. 1989 Jan;248(1):400-14; Neuroendocrinology. 1994 Nov;60(5):509-19. |
