Lazabemide 是一种单胺氧化酶 B 的选择性的可逆抑制剂 ,但对 MAO-A 活性较低。它高浓度时具有抑制单胺摄取的作用,能够抑制去甲肾上腺素、血清素和多巴胺摄取,其IC50值分别为 86 μM、123 μM 和 >500 μM。它可用于研究帕金森和阿尔茨海默病。
产品描述
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).
体外活性
LAZABEMIDE is selective, high-affinity ligands for enzymes.?KD and Bmax values for 3H-Ro 41 1049 in rat cerebral cortex were 10.7 nM and 7.38 pmol/mg protein, respectively, and for 3H-Ro 19 6327 were 18.4 nM and 3.45 pmol/mg protein, respectively.?In accordance with their potencies as enzyme inhibitors, binding to MAO-A and MAO-B was competitively inhibited by clorgyline (IC50 = 1.4 nM) and L-deprenyl (selegiline;?IC50 = 8.0 nM), respectively[1].
体内活性
Lazabemide is a reversible inhibitor of monoamine oxidase B (MAO-B) with IC50 values of 0.48 and 1.5 μM measured in platelets of human subjects ages 19-36 and 60-78, respectively[2].
Cas No.
103878-84-8
分子式
C8H10ClN3O
分子量
199.64
别名
拉扎贝胺;Ro 19-6327
储存和溶解度
DMSO:34 mg/mL (170.31 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years