天堂网亚洲,天天操天天搞,91视频高清,菠萝蜜视频在线观看入口,美女视频性感美女视频,95丝袜美女视频国产,超高清美女视频图片

返回ChemicalBook首頁>CAS數據庫列表>103878-84-8

103878-84-8

中文名稱 拉扎貝胺
英文名稱 LAZABEMIDE
CAS 103878-84-8
分子式 C8H10ClN3O
分子量 199.64
MOL 文件 103878-84-8.mol
更新日期 2024/12/03 15:40:37
103878-84-8 結構式 103878-84-8 結構式

基本信息

中文別名
拉扎貝胺
N-(2-氨基乙基)-5-氯-2-吡啶羧酰胺
英文別名
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
所屬類別
藥物: 中樞神經系統(tǒng)用藥: 抗癲癇藥

物理化學性質

外觀性狀單鹽酸拉扎貝胺(Lazabemide Monohydrochloride):C8Hl0ClN3O?HCl。[103878-83-7]。從甲醇-乙醚結晶,熔點193~195℃。分配系數(正辛醇脈):約0.1。pKa 8.9。急性毒性LD50小鼠(mg/kg):1000~2000口服。
沸點397.4±37.0 °C(Predicted)
密度1.286±0.06 g/cm3(Predicted)
儲存條件room temp
溶解度二甲基亞砜:≥22mg/mL
酸度系數(pKa)12.90±0.46(Predicted)
形態(tài)粉末
顏色白色至棕褐色

安全數據

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H319
危險品標志Xn
危險類別碼22-36
安全說明26
WGK Germany3

應用領域

用途1
抗帕金森病藥。為作用于腦內和外周器官的選擇性可逆的單胺氧化酶B(MAO-B)抑制劑。

制備方法

方法1
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,在四氫呋喃中回流,得到化合物(II)。再和三氟乙酸在二氯甲烷中回流水解,然后用乙醇鹽酸處理,得到單鹽酸拉扎貝胺。

常見問題列表

生物活性
Lazabemide (Ro 19-6327) 是單胺氧化酶 B (MAO-B) 的選擇性的可逆抑制劑 (IC50=0.03 μM),但對 MAO-A (IC50>100 μM) 活性較低。高濃度 Lazabemide 具有抑制單胺攝取的作用,抑制去甲腎上腺素、血清素和多巴胺攝取的 IC50 值分別為 86 μM、123 μM 和 >500 μM。Lazabemide 可用于帕金森和阿爾茨海默病的研究。
靶點

IC50: 30 nM (MAO-B).

體外研究

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.

體內研究

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.

"103878-84-8" 相關產品信息
25265-76-3 7696-12-0 191732-72-6