Moclobemide is a reversible inhibitor of monoamine oxidase type A; (RIMA); (see MONOAMINE OXIDASE INHIBITORS) that has antidepressive properties.

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. [1] 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. [2]

Moclobemide (10 mg/kg p.o.) induces a significant decrease of all monoamine metabolites measured in rat brain. [1] 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. [3] 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). [4] 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. [5]

71320-77-9

C13H17ClN2O2

268.74

吗氯贝胺;Ro111163;Moclobemide

[1]Girard P, et al. Can J Physiol Pharmacol, 2007, 85(5), 556-561.[2]Verleye M, et al. Brain Res, 2007, 1138, 30-38.[3]Cryan JF, et al. Psychopharmacology (Berl), 2005, 182(3), 335-344.[4]Reul JM, et al. Neuroendocrinology, 1994, 60(5), 509-519.[5]Da Prada M, et al. J Pharmacol Exp Ther, 1989, 248(1), 400-414.

Ethanol:26.9 mg/mL (100 mM)
DMSO:26.9 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years