优降宁盐酸盐
| 中文名称 | 优降宁盐酸盐 |
|---|---|
| 中文同义词 | 盐酸帕吉林;巴吉林,优降宁;MAO抑制剂(PARGYLINE HYDROCHLORIDE);巴吉林盐酸盐,丙炔甲基苄胺,巴吉林;巴吉林盐酸盐,丙炔甲基苄胺,帕吉林,巴吉林;N-甲基-N-2-丙炔基苄胺 盐酸盐;N-甲基-N-丙炔基苄胺 盐酸盐;优降宁 盐酸盐 |
| 英文名称 | PARGYLINE HYDROCHLORIDE |
| 英文同义词 | N-METHYL-N-PROPARGYLBENZYLAMINE HYDROCHLORIDE;N-METHYL-N-(2-PROPYNY)BENZYLAMINE HYDROCHLORIDE;N-METHYL-N-2-PROPYNYLBENZYLAMINE HYDROCHLORIDE;PARGYLINE HYDROCHLORIDE;benzylmethylpropynylaminehydrochloride;n-benzyl-n-methyl-2-propynylaminehydrochloride;n-benzyl-n-methyl-2-propynylaminhydrochloride;n-methyl-n-2-propynyl-benzylaminhydrochloride |
| CAS号 | 306-07-0 |
| 分子式 | C11H14ClN |
| 分子量 | 195.69 |
| EINECS号 | 206-175-1 |
| 相关类别 | 小分子抑制剂;细胞信号和神经生物学;细胞生物学;细胞生物学试剂;日用化学品;标准品;试剂 |
| Mol文件 | 306-07-0.mol |
| 结构式 |  |
优降宁盐酸盐 性质
| 熔点 | 160-163 °C(lit.) |
|---|---|
| 储存条件 | -20°C |
| 溶解度 | 乙醇中≥33.55 mg/mL；水中≥51.6 mg/mL； ≥7.55 mg/mL，溶于 DMSO |
| 形态 | 结晶固体 |
| 颜色 | 从EtOH/Et2O结晶的晶体 |
| 生物来源 | synthetic |
| 水溶解性 | water: 50mg/mL, clear, colorless to faintly yellow |
| Merck | 13,7110 |
| BRN | 3699487 |
| InChI | InChI=1S/C11H13N.ClH/c1-3-9-12(2)10-11-7-5-4-6-8-11;/h1,4-8H,9-10H2,2H3;1H |
| InChIKey | BCXCABRDBBWWGY-UHFFFAOYSA-N |
| SMILES | C1(=CC=CC=C1)CN(C)CC#C.Cl |
| CAS 数据库 | 306-07-0 |
| Target | Value |
|
MAO-B
(Cell-free assay) | 0.5 μM(Ki) |
|
MAO-A
(Cell-free assay) | 13 μM(Ki) |
Pargyline (0.5-2 mM; 24-120 hours; LNCaP-LN3 cells) treatment inhibits the proliferation of prostate cancer cells in a time- and dose-dependent manner.
Pargyline (0.5-2 mM; 24-48 hours; LNCaP-LN3 cells) treatment decreases S phase and increases the G1 phase in the cells in a dose-dependent manner.
Pargyline (0.5 mM; 24 hours; LNCaP-LN3 cells) treatment increases the apoptotic cells.
Pargyline (2 mM; 48 hours; LNCaP-LN3 cells) treatment induces an increase of cytochrome c and a decrease of caspase-3 in the cells, but does not lead to a change of BCL-2 expression.
Cell Proliferation Assay
| Cell Line: | LNCaP-LN3 cells |
| Concentration: | 0.5 mM, 1 mM, 1.5 mM or 2 mM |
| Incubation Time: | 24 hours, 48 hours, 72 hours, 96 hours or 120 hours |
| Result: | Inhibited the proliferation of prostate cancer cells in a time- and dose-dependent manner. |
Cell Cycle Analysis
| Cell Line: | LNCaP-LN3 cells |
| Concentration: | 0.5 mM, 2 mM |
| Incubation Time: | 24 hours, 48 hours |
| Result: | The S phase ratio of the cells was decreased, while their G1 phase ratio was increased. |
Apoptosis Analysis
| Cell Line: | LNCaP-LN3 cells |
| Concentration: | 0.5 mM |
| Incubation Time: | 24 hours |
| Result: | Increased the apoptotic cells. |
Western Blot Analysis
| Cell Line: | LNCaP-LN3 cells |
| Concentration: | 2 mM |
| Incubation Time: | 48 hours |
| Result: | Induced an increase of cytochrome c and a decrease of caspase-3. |
Pargyline (10 mg/kg; iv) treatment induces a moderate (about 20 mm Hg) but persistent (48 h) decrease of systolic blood pressure in unanesthetized adult spontaneously hypertensive rats (SHR) but not in normotensive rats.
A low dose of Pargyline (200 μg; icv) injected directly into the brain lowered arterial pressure. The hypotensive action of Pargylline in SHR appears to be the consequence of Norepinephrine accumulating at an inhibitory α-adrenoceptor in brain.
安全信息
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英文
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