Home Metabolism MAO inhibitor Moclobemide (Ro 111163)

research use only

Moclobemide (Ro 111163) MAO inhibitor

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

Purity & Quality Control

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

Related Products

Signaling Pathway

MAO Signaling Pathways

MAO Signaling Pathway

Mechanism of Action

Targets
MAO-A (5-HT) [1]
6.1 μM

In vitro
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. It also inhibits MAO-A and PEA in rat liver with ED50 of 8.4 μmol/kg and 6.6 μmol/kg, respectively. This compound (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] When included in the culture medium during anoxia or with glutamate at 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. [2]

In Vivo
In vivo Moclobemide (Ro 111163) (10 mg/kg p.o.) induces a significant decrease of all monoamine metabolites measured in rat brain. [1] 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 it (5 weeks, 4.5 mg/kg/day) significantly attenuates stress (30 min novel environment)-induced plasma ACTH (-35%) and corticosterone (-29%) levels. [3] At 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). [4] At 100 mg/kg/day, it combined with triethyltin blocks the development of brain edema and the increase in the cerebral chloride content induced by triethyltin in rats. This compound (100 mg/kg/day) reduces the increase in the cerebral sodium content and attenuates the neurological deficit in rats. [5]

References
  • https://pubmed.ncbi.nlm.nih.gov/2783611/
  • https://pubmed.ncbi.nlm.nih.gov/17274964/
  • https://pubmed.ncbi.nlm.nih.gov/7845541/
  • https://pubmed.ncbi.nlm.nih.gov/16001105/
  • https://pubmed.ncbi.nlm.nih.gov/17632591/

Chemical Information

Molecular Weight 268.74 Formula

C13H17ClN2O2
CAS No. 71320-77-9 SDF Download SDF
Synonyms N/A
Smiles C1COCCN1CCNC(=O)C2=CC=C(C=C2)Cl

Storage and Stability

Storage (From the date of receipt)

In vitro
Batch:

DMSO : 53 mg/mL ( (197.21 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.