MAO-B-IN-22

MAO-B-IN-22 (compound 6h) is a potent MAO-B inhibitor with an IC50 of 0.014 μM. MAO-B-IN-22 has high antioxidant activity, good metal chelating ability, proper BBB permeability and significant neuroprotective effect[1].

Signaling Pathways >> Neuronal Signaling >> Monoamine Oxidase

Research Areas >> Neurological Disease

MAO-B-IN-22 (compound 6h) (2.5-50 μM, 24 h) 可以剂量依赖性的保护过氧化氢诱导的氧化损伤，提高细胞活力[1]。 MAO-B-IN-22 (compound 6h) (0.5-10 μM, 24 h) 可以剂量依赖性的降低 LPS 诱导的 NO 产生，具有抗神经炎症活性[1]。 Cell Viability Assay[1] Cell Line: PC-12 cells Concentration: 2.5 μM, 10.0 μM, 50.0 μM Incubation Time: 24 h Result: Increased cell viability to 59.8%, 69.6% and 77.2% of the control value at doses of 2.5 μM, 10.0 μM and 50.0 μM, respectively. Western Blot Analysis[1] Cell Line: BV-2 cells Concentration: 0.5 μM, 2.5 μM, 10.0 μM Incubation Time: 24 h Result: Significantly reduced LPS-induced NO production by 13.5%, 28.0% and 76.1% at concentrations of 0.5 μM, 2.5 μM and 10.0 μM, respectively. Inhibited the release of ROS induced by lipopolysaccharide, and the inhibitory rates were 21.2% and 99.0% at the concentration of 2.5 μM and 10.0 μM , respectively. Significantly inhibited the phosphorylation of IκBα to p-IκBα, and inhibited the translocation of p65 from the cytoplasm to the nucleus.

MAO-B-IN-22 (compound 6h)(53.5 mg/kg, oral gavage, once a day for 3 weeks) 可以通过抑制 MAO-B 增加多巴胺能神经递质水平和减少 ROS 引起的氧化损伤水平来减轻小鼠的运动损伤，可以减轻 MPTP 治疗小鼠的运动障碍，并可能改善体内 PD 的症状[1]。 Animal Model: C57BL/6C mice[1] Dosage: 53.5 mg/kg Administration: oral gavage, once a day for 3 weeks Result: Significantly improved traction test scores and reduced BWT times, T-turns and T-totals. Restored DA levels and reduce MDA levels.

[1]. Zhongcheng Cao, et al. Discovery of novel 2-hydroxyl-4-benzyloxybenzyl aniline derivatives as potential multifunctional agents for the treatment of Parkinson's disease. Eur J Med Chem. 2023 Mar 5;249:115142.