拉扎贝胺盐酸盐

拉扎贝胺盐酸盐

中文名称拉扎贝胺盐酸盐
中文同义词拉扎贝胺盐酸盐;LAZABEMIDE盐酸盐
英文名称N-(2-Aminoethyl)-5-chlor-2-pyridincarboxamid-hydrochlorid
英文同义词N-(2-Aminoethyl)-5-chlor-2-pyridincarboxamid-hydrochlorid;2-PyridinecarboxaMide, N-(2-aMinoethyl)-5-chloro-, Monohydrochloride;Ro 19-6327/001;TeMpiuM;N-(2-Aminoethyl)-5-chloro-2-pyridinecarboxamide hydrochloride;JMFKTFLARGGXCC-UHFFFAOYSA-N;N-(2-Aminoethyl)-5-chlor-2-pyridincarbox;ichemia,Lazabemide,DOPAC,MAO,radical generation,Ro 19-6327,disease,alzheimer′s,Inhibitor,inhibit,Lazabemide hydrochloride,Monoamine Oxidase,smoking cessation,parkinson
CAS号103878-83-7
分子式C8H10ClN3O.HCl
分子量0
EINECS号
相关类别Monoamine Oxidase
Mol文件103878-83-7.mol
结构式拉扎贝胺盐酸盐 结构式

拉扎贝胺盐酸盐 性质

熔点193-195°
储存条件Desiccate at RT
溶解度在水中溶解度为 100 mM,在 DMSO 中溶解度为 100 mM
形态粉末
酸度系数(pKa)8.9(at 25℃)

拉扎贝胺盐酸盐 用途与合成方法

Lazabemide (Ro 19-6327)是可逆性、选择性MAO-B抑制剂,Ki值为7.9 nM。
TargetValue
MAO-B
(Cell-free assay)
7.9 nM(Ki)

The in vitro binding characteristics of both radiolabeled inhibitors revealed them to be selective, high-affinity ligands for the respective enzymes. K D and B max values for 3 H-Ro 19-6327 in rat cerebral cortex are 18.4 nM and 3.45 pmol/mg protein, respectively. The IC 50 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 IC 50 of 6.9 nM and >10 nM, respectively. And it inhibits rat MAO-B and MAO-A with IC 50 of 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 not increase 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.

安全信息

毒性LD50 orally in mice: 1000-2000 mg/kg (Imhof, Kyburz, 1986)

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/08/19S6422拉扎贝胺盐酸盐
Lazabemide
103878-83-725mg1286.7元

拉扎贝胺盐酸盐 上下游产品信息

"拉扎贝胺盐酸盐"相关产品信息
甲胺盐酸盐 半胱胺盐酸盐 N-甲基-1-吡啶-2-甲胺 5-氯吡啶-2-醛 拉扎贝胺 拉扎贝胺盐酸盐
主页 | 企业会员服务 | 广告业务 | 联系我们 | 旧版入口 | 中文MSDS | CAS Index | 常用化学品CAS列表 | 化工产品目录 | 新产品列表 | 评选活动 | HS海关编码 | MSDS查询 | 化工站点

Copyright © 2016-2023 ChemicalBook 版权所有  京ICP备07040585号  京公海网安备11010802032676号  

互联网增值电信业务经营许可证:京ICP证150597号  互联网药品信息服务资格证编号(京)-非经营性-2015-0073  信息系统安全等级保护备案证明(三级)  营业执照公示

根据相关法律法规和本站规定,单位或个人购买相关危险物品应取得有效的资质、资格条件。
参考《应急管理部等多部门关于加强互联网销售危险化学品安全管理的通知 (应急〔2022〕119号)》《互联网危险物品信息发布管理规定》