LAZABEMIDE

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LAZABEMIDE(Ro 19-6327) 是一种选择性、可逆单胺氧化酶 B (MAO-B) 抑制剂（MAO-B 和 MAO-A 的 IC50 值分别为 0.03 和 > 100 μM）。

LAZABEMIDE(Ro 19-6327) is selective reversible monoamine oxidase B (MAO-B) inhibitor (IC50 values are 0.03 and > 100 μM for MAO-B and MAO-A respectively).

The in vitro binding characteristics of both radiolabeled inhibitors revealed them to be selective, high-affinity ligands for the respective enzymes. KD and Bmaxvalues 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 notincrease the accumulation of newly-formed DA in those tubular epithelial cells loaded with 50 microM L-DOPA.

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.

Ro 19-6327

Metabolic Enzyme/Protease

MAO

MAO-B

——

——

103878-84-8

199.64

C8H10ClN3O

>98% (HPLC)

DMSO:34 mg/mL (170.31 mM)

NCCNC(=O)c1ccc(Cl)cn1

Cyclopent(b)indole-3-acetic acid 4-((4-chlorophenyl)methyl)-7-fluoro-1234-tetrahydro-5-(methylsulfonyl)- (3R)-

(-20℃)

With Ice Pack

≥ 2 years