KDS2010 is a highly selective, substrate-competitive, potent and reversible monoamine oxidase MAO-B inhibitor (IC50 = 7.6 nM/MAO-B vs >100 μM/MAO-A; little affinity toward 99 kinases and 84 non-kinase targets) with excellent ADME/Tox profiles (IC50 >10 μM/P450, >50 μM/hERG), brain permeability and oral availability ([rat F = 123.5%; 10 mg/kg p.o.). KDS2010 restores memory impairments in APP/PS1 mice following either short- or long-term treatment (3-d or 4-wk 10 mg/kg/day p.o.) without aberrant GABA levels observed with prolonged irreversible inhibition by selegiline (MAO-B/MAO-A IC50 = 10 nM/1.5 μM) due to compensatory diamine oxidase (DAO) induction.
Orally active, brain-penetrant, highly selective, potent, reversible MAO-B inhibitor without aberrant GABA levels observed with long-term selegiline treatment in AD mice.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Monoamine oxidase-B (MAO-B) has recently emerged as a potential therapeutic target for Alzheimer's disease (AD) because of its association with aberrant γ-aminobutyric acid (GABA) production in reactive astrocytes. Although short-term treatment with irreversible MAO-B inhibitors, such as selegiline, improves cognitive
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