优降宁盐酸盐

生物活性靶点体外研究体内研究优降宁盐酸盐试剂级价格

优降宁盐酸盐

CAS号:306-07-0
英文名:PARGYLINE HYDROCHLORIDE
中文名:优降宁盐酸盐
CBNumber:CB0436582
分子式:C11H14ClN
分子量:195.69
MOL File:306-07-0.mol

优降宁盐酸盐化学性质

熔点 :160-163 °C(lit.)
储存条件 :-20°C
溶解度 :≥33.55 mg/mL in EtOH; ≥51.6 mg/mL in H2O; ≥7.55 mg/mL in DMSO
形态 :A crystalline solid
颜色 :Crystals from EtOH/Et2O
Merck :13,7110
BRN :3699487
InChIKey :BCXCABRDBBWWGY-UHFFFAOYSA-N
CAS 数据库 :306-07-0

安全信息

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
F :10
危险等级 :6.1(b)
包装类别 :III
海关编码 :2921199990
毒性 :LD50 orl-rat: 250 mg/kg 27ZQAG -,401,72

优降宁盐酸盐性质、用途与生产工艺

生物活性 Pargyline hydrochloride 是一种不可逆的单胺氧化酶 (MAO) 抑制剂，对 MAO-A 和 MAO-B 的 Ki 分别为 13 μM 和 0.5 μM。Pargyline hydrochloride 具有降压和抗癌活性。
靶点
Target Value
MAO-B
(Cell-free assay) 0.5 μM(Ki)
MAO-A
(Cell-free assay) 13 μM(Ki)

体外研究

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.

体内研究

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.
用途具有明显的降压作用，单胺氧化酶(MAO-B)选择性抑制剂。
类别有毒物品
毒性分级高毒
急性毒性口服-大鼠 LD50: 142 毫克/公斤; 口服-小鼠 LD50; 680 毫克/公斤
可燃性危险特性可燃;燃烧产生有毒氮氧化物和氯化氢烟雾;药物副作用:影响心理状态;影响液体吸收
储运特性通风低温干燥; 与库房食品原料分开存放
灭火剂干粉,泡沫,沙土,二氧化碳, 雾状水