M 30 dihydrochloride

MAO-IN-M30 dihydrochloride is an orally active, brain-permeable, and brain selective irreversible MAO-A (IC50=37 nM) and MAO-B (IC50=57 nM) inhibitor. MAO-IN-M30 dihydrochloride is a potent iron chelator and radical scavenger. MAO-IN-M30 dihydrochloride has a neuroprotective effect against Dexamethasone-induced brain cell apoptosis. MAO-IN-M30 dihydrochloride also exhibits neurorestorative activity in post MPTP and lactacystin models of Parkinson's disease[1][2][3].

Signaling Pathways >> Neuronal Signaling >> Monoamine Oxidase

Research Areas >> Neurological Disease

MAO-A:37 nM (IC50)

MAO-B:57 nM (IC50)

MAO-IN-M30 (0.25 nM; 72 hours) significantly increased cell viability to ~90% after exposure to Dexamethasone[3]. MAO-IN-M30 (0-10 μM; 24 hours) enhances PC12 cell survival[4]. MAO-IN-M30 treatment significantly decreases the occurrence of fragmented DNA compared to the dexamethasone-treated group in SH-SY5Y cells[3]. Cell Viability Assay[3] Cell Line: SH-SY5Y cells Concentration: 0.25 nM Incubation Time: 72 hours Result: Significantly increased cell viability to ∼90% after exposure to Dexamethasone. Cell Viability Assay[4] Cell Line: PC12 cells Concentration: 0-10 μM Incubation Time: 24 hours Result: Enhanced the PC12 cell viability, the cell viability increasing to 85 ± 6 and 90 ± 7%.

MAO-IN-M30 (0.5-2.5 mg/kg; p.o.; once daily for 14 consecutive days) possesses neuroprotective activities[6]. Animal Model: Male C57/BL mice (20-22 g; MPTP-induced neurotoxicity in mice)[6] Dosage: 0.5, 2.5 mg/kg Administration: P.o.; once daily for 14 consecutive days Result: Significantly elevate striatal dopamine levels, reduce its metabolism, and elevate tyrosine-hydroxylase protein levels and activity. Elevated MPTP-reduced dopaminergic and transferrin receptor cell count in the SNpc.

[1]. Gal S, et al. M30, a novel multifunctional neuroprotective drug with potent iron chelating and brain selective monoamine oxidase-ab inhibitory activity for Parkinson's disease. J Neural Transm Suppl. 2006;(70):447-456.

[2]. Zheng H, et al. Novel multifunctional neuroprotective iron chelator-monoamine oxidase inhibitor drugs for neurodegenerative diseases: in vitro studies on antioxidant activity, prevention of lipid peroxide formation and monoamine oxidase inhibition. J Neurochem. 2005;95(1):68-78.

[3]. Gal S, et al. Novel multifunctional neuroprotective iron chelator-monoamine oxidase inhibitor drugs for neurodegenerative diseases. In vivo selective brain monoamine oxidase inhibition and prevention of MPTP-induced striatal dopamine depletion. J Neurochem. 2005;95(1):79-88.

[4]. Gal S, et al. Restoration of nigrostriatal dopamine neurons in post-MPTP treatment by the novel multifunctional brain-permeable iron chelator-monoamine oxidase inhibitor drug, M30. Neurotox Res. 2010;17(1):15-27.