MAO-B-IN-7 is a potent and blood-brain barrier permeable MAO-B and AChE inhibitor, exhibiting IC50 values of 41 nM for human AChE, 87 nM for electric eel AChE, and 0.3 μM for MAO-B. MAO-B-IN-7 effectively alleviates oxidative stress and neuroinflammatory damage.

MAO-B:0.3 μM, AChE (human):41 nM

MAO-B-IN-7 (compound 7d) interacts with Cu 2+ to form complexes and strongly inhibits Cu 2+-induced ROS production. At concentrations of 10-100 µM over 24 hours, it reduces the viability of PC-12 cells at 100 µM, with minimal cytotoxicity at 10-25 µM. It protects PC-12 cells from H2O2-induced injury, yielding viability percentages of 80.2%, 71.1%, and 56.3% at 25.0 µM, 10.0 µM, and 4.0 µM. At 2.5 µM and 10 µM for 8 and 24 hours, it dose-dependently inhibits LPS-induced ROS in BV-2 cells, reduces NO production by 30.4%, 43.5%, and 58.9%, and decreases TNF-α release by 32.7%, 47.8%, and 63.2% at 0.5 µM, 2.5 µM, and 10.0 µM. Additionally, MAO-B-IN-7 demonstrates a parallel artificial membrane permeation of 8.59 × 10^-6 in in vitro blood-brain barrier studies.