Moclobemide

SKU: orb1310956

Description

Moclobemide is a reversible inhibitor of monoamine oxidase A (RIMA) with antidepressant properties. It is used in research to study depression mechanisms and has been utilized in both in vitro enzyme assays and in vivo animal models of depressive-like behavior.

Research Area

Metabolism Research, Neuroscience

Key Properties

• CAS Number: 71320-77-9
• MW: 268.74
• Purity: 99.51%
• Formula: C₁₃H₁₇ClN₂O₂
• SMILES: ClC1=CC=C(C=C1)C(=O)NCCN1CCOCC1
• Target: Monoamine Oxidase,MAO
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (7.44 mM);Ethanol:26.9 mg/mL (100.1 mM);DMSO:65 mg/mL (241.87 mM)

Bioactivity

• Target IC50:
  MAO-A:6.1 μM
• 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.
• In Vitro:
  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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

brain-derived, antidepressants, MAO-A (5-HT), MAO, hippocampal, inhibit, Inhibitor, monoamine, Monoamine Oxidase, MonoamineOxidase, neurogenesis, neurotrophic, Moclobemide, oxidase,MAO-A, stress, Ro 111163, Ro111163, Ro-111163, progenitor

Compound Identifiers

PubChem CID

4235