CAS NO: | 103878-83-7 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
生物活性 | Lazabemide hydrochloride (Ro 19-6327 hydrochloride) is a selective, reversible inhibitor ofmonoamine oxidaseB (MAO-B)(IC50=0.03 μM) but less active forMAO-A(IC50>100 μM). Lazabemide inhibits monoamine uptake at high concentrations, the IC50values 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] |
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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. KDand Bmaxvalues for3H-Ro 19-6327 in rat cerebral cortex are 18.4 nM and 3.45 pmol/mg protein, respectively[1].The IC50values 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 IC50of 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]. | |
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]. | |
分子量 | 236.10 | |
Formula | C8H11Cl2N3O | |
CAS 号 | 103878-83-7 | |
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. |