1. Neuronal Signaling
  2. Monoamine Oxidase
  3. Lazabemide hydrochloride

Lazabemide hydrochloride  (Synonyms: Ro 19-6327 hydrochloride)

目录号: HY-14202
产品使用指南

Lazabemide hydrochloride (Ro 19-6327 hydrochloride) 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。

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Lazabemide hydrochloride Chemical Structure

Lazabemide hydrochloride Chemical Structure

CAS No. : 103878-83-7

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生物活性

Lazabemide hydrochloride (Ro 19-6327 hydrochloride) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide  inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and alzheimer′s disease[1].

IC50 & Target[1]

MAO-B

0.4 nM (IC50)

体外研究
(In Vitro)

The in vitro binding characteristics of both radiolabeled inhibitors revealed them to be selective, high-affinity ligands for the respective enzymes. KD and Bmax values for 3H-Ro 19-6327 in rat cerebral cortex are 18.4 nM and 3.45 pmol/mg protein, respectively[1].
The IC50 values for lazabemide are: 86 μM for NA uptake; 123 μM for 5HT uptake; > 500 μM for DA uptake, respectively[1].
. 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[2].
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[2].
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[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

236.10

Formula

C8H11Cl2N3O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

Lazabemide hydrochloride 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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