拉扎贝胺
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- CAS号:
- 103878-84-8
- 英文名:
- LAZABEMIDE
- 英文别名:
- Ro-19-6327;LAZABEMIDE;Ro 19-6327/000;Lazabemide hydrate;Ro 19-6327 hydrate;LAZABEMIDE HYDROCHLORIDE;N-(2-aminoethyl)-5-chloropyridine-2-carboxamide;N-(2-Aminoethyl)-5-chloro-2-pyridinecarboxamide;2-PyridinecarboxaMide, N-(2-aMinoethyl)-5-chloro-;N-(2-Aminoethyl)-5-chloro-2-pyridinecarboxamide hydrate
- 中文名:
- 拉扎贝胺
- 中文别名:
- 拉扎贝胺;N-(2-氨基乙基)-5-氯-2-吡啶羧酰胺
- CBNumber:
- CB6149051
- 分子式:
- C8H10ClN3O
- 分子量:
- 199.64
- MOL File:
- 103878-84-8.mol
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拉扎贝胺化学性质
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沸点:
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397.4±37.0 °C(Predicted)
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密度:
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1.286±0.06 g/cm3(Predicted)
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储存条件:
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room temp
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溶解度:
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DMSO: ≥22mg/mL
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酸度系数(pKa):
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12.90±0.46(Predicted)
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形态:
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powder
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颜色:
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white to tan
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拉扎贝胺性质、用途与生产工艺
Lazabemide (Ro 19-6327) 是单胺氧化酶 B (MAO-B) 的选择性的可逆抑制剂 (IC50=0.03 μM)，但对 MAO-A (IC50>100 μM) 活性较低。高浓度 Lazabemide 具有抑制单胺摄取的作用，抑制去甲肾上腺素、血清素和多巴胺摄取的 IC50 值分别为 86 μM、123 μM 和 >500 μM。Lazabemide 可用于帕金森和阿尔茨海默病的研究。
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.
化学性质
单盐酸拉扎贝胺(Lazabemide Monohydrochloride)：C8Hl0ClN3O?HCl。[103878-83-7]。从甲醇-乙醚结晶，熔点193～195℃。分配系数(正辛醇脉)：约0.1。pKa 8.9。急性毒性LD
50小鼠(mg/kg)：1000~2000口服。
用途
抗帕金森病药。为作用于脑内和外周器官的选择性可逆的单胺氧化酶B(MAO-B)抑制剂。
生产方法
5-氯吡啶2-羧酸(I)和N-(2-氨基乙基)氨基甲酸叔丁酯(Ⅱ)，在羰二咪唑(CDI)存在下，在四氢呋喃中回流，得到化合物(II)。再和三氟乙酸在二氯甲烷中回流水解，然后用乙醇盐酸处理，得到单盐酸拉扎贝胺。
拉扎贝胺
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 |
|---|
| 2024/01/25 | HY-14201 | Lazabemide | | 5 mg | 312元 |
| 2024/01/25 | HY-14201 | 拉扎贝胺
Lazabemide | 103878-84-8 | 10mg | 500元 |
拉扎贝胺
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拉扎贝胺国内生产厂家
103878-84-8, 拉扎贝胺 相关搜索:
- 合成有机化合物配体
- 原料药
- 中枢神经系统用药
- 药物
- 抗癫痫药
- N-(2-氨基乙基)-5-氯-2-吡啶羧酰胺
- 拉扎贝胺
- 103878-84-8
- N-(2-aminoethyl)-5-chloropyridine-2-carboxamide
- Ro 19-6327 hydrate
- N-(2-Aminoethyl)-5-chloro-2-pyridinecarboxamide hydrate
- Lazabemide hydrate
- Ro 19-6327/000
- 2-PyridinecarboxaMide, N-(2-aMinoethyl)-5-chloro-
- Ro-19-6327
- N-(2-Aminoethyl)-5-chloro-2-pyridinecarboxamide
- LAZABEMIDE HYDROCHLORIDE
- LAZABEMIDE