盐酸帕吉林 pargyline hydrochloride CAS#:306-07-0

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氯化钾 | 乙二醇 | 碘甲烷 | 溴化亚铜 | 叔丁醇钾 | DMAP

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首页化工产品目录原料药循环系统用药抗高血压病药盐酸帕吉林

盐酸帕吉林

产品纠错

CAS号：306-07-0 | 英文名称：pargyline hydrochloride

分子式 C₁₁H₁₄ClN

分子量 196

EINECS号 206-175-1

MDL MFCD00012492

Smiles C1(=CC=CC=C1)CN(C)CC#C.Cl

InChIKey BCXCABRDBBWWGY-UHFFFAOYSA-N

乙二醇化学百科

基本信息

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

物化性质

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
Merck	13,7110
BRN	3699487

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
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

生产及用途

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