Moclobemide (Ro 111163)

- Overview
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    Background
    
    Moclobemide is a reversible inhibitor of monoamine oxidase-A (MAO-A) with IC50 value of 10μM [1].
    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 [2].
    
    [1] Pisani L, Barletta M, Soto-Otero R, Nicolotti O, Mendez-Alvarez E, Catto M, Introcaso A, Stefanachi A, Cellamare S, Altomare C, Carotti A. Discovery, biological evaluation, and structure-activity and -selectivity relationships of 6'-substituted (E)-2-(benzofuran-3(2H)-ylidene)-N-methylacetamides, a novel class of potent and selective monoamine oxidase inhibitors. J Med Chem. 2013 Mar 28;56(6):2651-64.
    [2] Nair NP, Ahmed SK, Kin NM. Biochemistry and pharmacology of reversible inhibitors of MAO-A agents: focus on moclobemide. J Psychiatry Neurosci. 1993 Nov;18(5):214-25.
- Properties
  - Alternative Name
    
    4-chloro-N-(2-morpholin-4-ylethyl)benzamide
    
    CAS Number
    
    71320-77-9
    
    Molecular Formula
    
    C13H17ClN2O2
    
    Molecular Weight
    
    268.74
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥48.3 mg/mL in EtOH with ultrasonic; ≥9.85 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Moclobemide (Ro 111163)

Background

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