| 中文名称 | 优降宁盐酸盐 |
| 英文名称 | PARGYLINE HYDROCHLORIDE |
| CAS号 | 306-07-0 |
| 分子式 | C11H14ClN |
| 分子量 | 195.69 |
| EINECS号 | 206-175-1 |
| 熔点 | 160-163 °C(lit.) |
| 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 |
| 默克索引编号 | 13,7110 |
| BRN | 3699487 |
| 危险品标志 | Xn |
| 危险类别码 | 22 |
| 安全说明 | 22-24/25 |
| 危险品运输编号 | UN 2811 6.1/PG 3 |
| WGK Germany | 3 |
| RTECS号 | DP6650000 |
| 海关编码 | 2921199990 |
| 危险等级 | 6.1(b) |
| 包装类别 | III |
| 毒性 | LD50 orl-rat: 250 mg/kg 27ZQAG -,401,72 |
| 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.
