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CAS No. : 120635-25-8
MCE 国际站:Mofegiline hydrochloride
产品活性:Mofegiline hydrochloride (MDL72974A) 是一种靶向 MAO-B,酶激活不可逆的抑制剂,具有口服活性和选择性。Mofegiline hydrochloride 对 MAO-A 和 MAO-B 的 IC50 分别为 680 nM 和 3.6 nM。Mofegiline hydrochloride 也是一种氨基脲敏感胺氧化酶 (SSAO) 的抑制剂。
研究领域:Neuronal Signaling
作用靶点:Monoamine Oxidase
In Vitro: Mofegiline hydrochloride (MDL72974A) inhibits rat brain mitochondrial MAO in a concentration and time-dependent fashion.
Mofegiline hydrochloride (MDL72974A) inhibits [3H]dopamine (15 nM) uptake with an IC50 value of 31.8 μM, but poorly inhibits [3H]GBR-12935 (1 nM) binding (IC50 >100 μM) in the rat striatum.
Mofegiline hydrochloride (MDL72974A) inhibits SSAOs from dog aorta, rat aorta, bovine aorta and human umbilical artery with IC50s of 2 nM, 5 nM, 80 nM and 20 nM, respectively.
In Vivo: Mofegiline hydrochloride (MDL72974A) (0.1-2.5 mg/kg; p.o.; single dose) inhibits MAO-B activity external vivo in rat model and (1.25 mg/kg; i.p.; 18 hours prior to MPTP treatment) exerts its ability to block MPTP neurotoxicity in mice model.
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