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MAO-A/5-HT2AR-IN-1

CAS No. : 2769156-00-3

MCE 站：MAO-A/5-HT2AR-IN-1

产品活性：MAO-A/5-HT2AR-IN-1 (compound I14) 是一种有效的 MAO-A 和 5-HT2AR 双重抑制剂，其 IC ₅₀ 分别为 0.004 和 0.014 μM。MAO-A/5-HT2AR-IN-1 是一种潜在的抗抑郁剂。

研究领域：Neuronal Signaling  |  GPCR/G Protein

作用靶点：Monoamine Oxidase  |  5-HT Receptor

In Vitro: MAO-A/5-HT2AR-IN-1 (compound I14) (0-4 μM, 24 h) exhibits a significant neurocytoprotective effect on the CORT-induced cell depression model.
MAO-A/5-HT2AR-IN-1 is able to occupy the active cavity of 5-HT2AR ａnd MAO-A with multiple hydrogen bonding forces ａnd ππ stacking interaction.
MAO-A/5-HT2AR-IN-1 exhibits low proliferation inhibitory activities against L02 cells (IC₅₀ > 100 μM), SH-SY5Y (IC₅₀ > 10 μM) ａnd PC12 (IC₅₀ > 10 μM), indicating it has a good safety profile.

In Vivo: MAO-A/5-HT2AR-IN-1 (compound I14) (10 ａnd 20 mg/kg) significantly ameliorates the depression-like behavior of mice.
MAO-A/5-HT2AR-IN-1 (0-1 μM, for 7 days) improves zebrafish locomotion ａnd the depression-like behavior.
MAO-A/5-HT2AR-IN-1 is able to repair the damage of mice hippocampal neuronal cells ａnd reduce the expression of 5-HT2AR in mice brain tissue.
MAO-A/5-HT2AR-IN-1 (2 mg/kg (i.v.) 10 mg/kg (i.g.); once) has a good clearance rate of 345.69 mL/min/kg in rats.

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