N-(2-Aminoethyl)-5-chlor-2-pyridincarbox

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

N-(2-氨基乙基)-5-氯-2-吡啶羧基是一种可逆、选择性的mao-b抑制剂(Ki：7.9nM)。

N-(2-Aminoethyl)-5-chlor-2-pyridincarbox is a reversible and selective mao-b inhibitor(Ki：7.9nM).

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.

Lazabemide hydrochloride

Metabolic Enzyme/Protease

MAO

MAO-B

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103878-83-7

236.1

C8H11Cl2N3O

>98% (HPLC)

DMSO:40 mg/mL (169.42 mM)

Cl.NCCNC(=O)c1ccc(Cl)cn1

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(-20℃)

With Ice Pack

≥ 2 years