拉扎贝胺盐酸盐
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- CAS号:
- 103878-83-7
- 英文名:
- N-(2-Aminoethyl)-5-chlor-2-pyridincarboxamid-hydrochlorid
- 英文别名:
- TeMpiuM;Ro 19-6327/001;JMFKTFLARGGXCC-UHFFFAOYSA-N;N-(2-Aminoethyl)-5-chlor-2-pyridincarbox;N-(2-Aminoethyl)-5-chlor-2-pyridincarboxamid-hydrochlorid;N-(2-Aminoethyl)-5-chloro-2-pyridinecarboxamide hydrochloride;2-PyridinecarboxaMide, N-(2-aMinoethyl)-5-chloro-, Monohydrochloride;ichemia,Lazabemide,DOPAC,MAO,radical generation,Ro 19-6327,disease,alzheimer′s,Inhibitor,inhibit,Lazabemide hydrochloride,Monoamine Oxidase,smoking cessation,parkinson
- 中文名:
- 拉扎贝胺盐酸盐
- 中文别名:
- 拉扎贝胺盐酸盐;LAZABEMIDE盐酸盐
- CBNumber:
- CB11448718
- 分子式:
- C8H10ClN3O.HCl
- 分子量:
- 0
- MOL File:
- 103878-83-7.mol
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拉扎贝胺盐酸盐化学性质
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熔点:
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193-195°
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储存条件:
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Desiccate at RT
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溶解度:
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Soluble to 100 mM in water and to 100 mM in DMSO
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形态:
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Powder
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酸度系数(pKa):
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8.9(at 25℃)
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拉扎贝胺盐酸盐性质、用途与生产工艺
Lazabemide (Ro 19-6327)是可逆性、选择性MAO-B抑制剂，Ki值为7.9 nM。
| Target | Value |
MAO-B
(Cell-free assay)
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7.9 nM(Ki)
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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.
拉扎贝胺盐酸盐
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | S6422 | 拉扎贝胺盐酸盐
Lazabemide | 103878-83-7 | 25mg | 1286.7元 |
103878-83-7, 拉扎贝胺盐酸盐 相关搜索:
- Monoamine Oxidase
- 药靶配体
- C8H10ClN3OHCl
- LAZABEMIDE盐酸盐
- 拉扎贝胺盐酸盐
- 103878-83-7
- ichemia,Lazabemide,DOPAC,MAO,radical generation,Ro 19-6327,disease,alzheimer′s,Inhibitor,inhibit,Lazabemide hydrochloride,Monoamine Oxidase,smoking cessation,parkinson
- N-(2-Aminoethyl)-5-chlor-2-pyridincarbox
- JMFKTFLARGGXCC-UHFFFAOYSA-N
- N-(2-Aminoethyl)-5-chloro-2-pyridinecarboxamide hydrochloride
- TeMpiuM
- Ro 19-6327/001
- 2-PyridinecarboxaMide, N-(2-aMinoethyl)-5-chloro-, Monohydrochloride
- N-(2-Aminoethyl)-5-chlor-2-pyridincarboxamid-hydrochlorid