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Lazabemide

CAS No. : 103878-84-8

MCE 站：Lazabemide

产品活性：Lazabemide (Ro 19-6327) 是单胺氧化酶 B (MAO-B) 的选择性的可逆抑制剂 (IC₅₀=0.03 μM)，但对 MAO-A (IC₅₀>100 μM) 活性较低。高浓度 Lazabemide 具有抑制单胺摄取的作用，抑制去甲肾上腺素、血清素和多巴胺摄取的 IC₅₀ 值分别为 86 μM、123 μM 和 >500 μM。Lazabemide 可用于帕金森和阿尔茨海默病的研究。

研究领域：Neuronal Signaling

作用靶点：Monoamine Oxidase

In Vitro: The in vitro binding characteristics of both radiolabeled inhibitors revealed them to be selective, high-affinity ligands for the respective enzymes. K_D and B_max values for ³H-Ro 19-6327 in rat cerebral cortex are 18.4 nM and 3.45 pmol/mg protein, respectively.
The IC₅₀ values for lazabemide are: 86 μM for NA uptake; 123 μM for 5HT uptake; > 500 μM for DA uptake, respectively.
. Lazabemide (5 μM) inhibits human MAO-B and MAO-A with IC₅₀ of 6.9 nM and >10 nM, respectively. And it inhibits rat MAO-B and MAO-A with IC₅₀of 37 nM and >10 μM, respectively ina enzymatic assay.
Lazabemide differs from L-deprenyl in their ability to induce release of endogenous monoamines from synaptosomes. Thus, Lazabemide (500 μM) induces a greater 5 HT release than does L-deprenyl, but is less effective than L-deprenyl in releasing DA. On the contrary, lazabemide was almost completely inactive on either 5-HT and DA release.
Lazabemide (250 nM) results in a clear inhibition of DOPAC formation, while does not increase the accumulation of newly-formed DA in those tubular epithelial cells loaded with 50 microM L-DOPA.

In Vivo: Lazabemide (3 mg/kg) attenuates ichemia reperfusion-induced hydroxyl radical generation and pretreatment with Lazabemide showed decreased DOPAC levels in comparison with those of their respective vehicle-treated control groups.

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