Mofegiline
Mofegiline (MDL-72974) is an orally active and blood-brain barrier-penetrant MAO-B/SSAO selective inhibitor, with an IC50 of 3.6 nM for MAO-B and 10 nM for SSAO. Mofegiline is a cationic amphiphilic compound that can induce indirect sympathomimetic effects, lysosomal accumulation, hERG channel interactions, phospholipidosis, and cell death. Mofegiline protects mice from MPTP-induced depletion of striatal dopamine, DOPAC, and HVA. Mofegiline can be used in research related to Parkinson's disease.
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- CAS No.: 119386-96-8
- Formule: C11H13F2N
- Masse moléculaire:197.23
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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- Pureté et documentation
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Activité biologique
Description
IC50 & Target
[1]|
MAO-B 3.6 nM (IC50) |
MAO-A |
In Vitro
Mofegiline (compound 1) is a potent dual inhibitor of SSAO (IC50 = 0.010 μM) and MAO-B (IC50 = 0.002 μM) in cell-free amine oxidase assays, with selectivity over MAO-A (IC50 = 0.75 μM) and DAO (IC50 >30 μM); it also produces phospholipidosis/cytotoxicity risk in vitro[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Mofegiline (1.25 mg/kg; i.p.; single dose; before MPTP) prevents MPTP-induced depletion of striatal dopamine, DOPAC, and HVA in mice[1].
Mofegiline (escalating doses; i.v.) produced only minor indirect sympathomimetic cardiovascular effects in pithed rats and did not potentiate the tyramine response[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss-Webster (CF-W) (male, 25-30 g)[1]
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Dosage:1.25 mg/kg
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Administration:i.p.; once; 18 hours prior to MPTP (HY-W114750)
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Result:Prevented MPTP-induced depletion of striatal dopamine, DOPAC, and HVA in mice.
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Animal Model:Sprague-Dawley (male, 150-400 g)[1]
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Dosage:1.8 mg/kg and 9 mg/kg (acute)
0.1 mg/kg or 1 mg/kg (chronic) -
Administration:p.o.; acute or daily
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Result:Did not significantly potentiate the cardiovascular effects of intraduodenally administered tyramine in anaesthetized rats, even at 9 mg/kg acute, which was 50 times the brain MAO-B ED50 of 0.18 mg/kg.
Daily administration at 1 mg/kg, which was 40 times the brain MAO-B ED50, did not potentiate the cardiovascular effects of intraduodenally administered tyramine.
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Animal Model:Wistar rats (Male, 200 250 g) received daily injections of either saline, 0.01 or 0.04 mg/kg Pergolide (HY-13720) or saline[3]
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Dosage:1.25, 25 mg/kg
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Administration:i.p.; daily; 3 weeks
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Result:At 1.25 mg/kg, striatal CuZn SOD activity was 102%.
At 25 mg/kg, striatal CuZn SOD activity was 97%.
Had no effect on CuZn SOD at either dose.
Chemical Information
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CAS No. 119386-96-8
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Masse moléculaire 197.23
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Formule C11H13F2N
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SMILES
C(C/C(=C\F)/CN)C1=CC=C(F)C=C1
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Synonyms
MDL-72974
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Mofegiline Related Classifications
HY-16677 Related Classifications
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