Home Metabolism MAO inhibitor Moclobemide (Ro 111163)

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Moclobemide (Ro 111163) MAO inhibitor

Cat.No.S3212

Moclobemide (Ro 111163) is a MAO-A (5-HT) inhibitor with IC50 of 6.1 μM.
Moclobemide (Ro 111163) MAO inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 268.74

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Quality Control

Batch: S321201 DMSO]53 mg/mL]false]Ethanol]10 mg/mL]false]Water]Insoluble]false Purity: 99.81%
99.81

Solubility

In vitro
Batch:

DMSO : 53 mg/mL (197.21 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 268.74 Formula

C13H17ClN2O2

 Storage (From the date of receipt)
CAS No. 71320-77-9 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1COCCN1CCNC(=O)C2=CC=C(C=C2)Cl

Mechanism of Action

Targets/IC50/Ki
MAO-A (5-HT)
6.1 μM
In vitro
Moclobemide (Ro 111163), when 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. This compound also inhibits MAO-A and PEA in rat liver with ED50 of 8.4 μmol/kg and 6.6 μmol/kg, respectively, under the same conditions. In vitro, it (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. When included in the culture medium during anoxia or with glutamate at concentrations of 10 mM-100 mM, it 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 (Ro 111163) (10 mg/kg p.o.) induces a significant decrease of all monoamine metabolites measured in rat brain. When given via the drinking water (4.5 mg/kg/day), this compound produces significant decreases in adrenal weight of rats after 5 (-23%) and 7 weeks (-16%) of treatment. It 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. Treatment with this agent (5 weeks, 4.5 mg/kg/day) significantly attenuates stress (30 min novel environment)-induced plasma ACTH (-35%) and corticosterone (-29%) levels. At a dosage of 2.5 mg/kg/day, it 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. When administered at 15 mg/kg/day, it decreased immobility and increased swimming for 3 days, whereas treatment for 14 days significantly increases both active behavior (swimming and climbing). At 100 mg/kg/day, this compound combined with triethyltin blocks the development of brain edema and the increase in the cerebral chloride content induced by triethyltin in rats. It also reduces the increase in the cerebral sodium content and attenuates the neurological deficit in rats.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/16001105/
  • [5] https://pubmed.ncbi.nlm.nih.gov/17632591/

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