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306-07-0

中文名称 巴吉林,优降宁
英文名称 PARGYLINE HYDROCHLORIDE
CAS 306-07-0
分子式 C11H14ClN
分子量 195.69
MOL 文件 306-07-0.mol
更新日期 2024/04/22 18:17:48
306-07-0 结构式 306-07-0 结构式

基本信息

中文别名
盐酸帕吉林
丙炔甲基苄胺
巴吉林盐酸盐
巴吉林,优降宁
优降宁 盐酸盐
盐酸帕吉林 标准品
N-甲基-N-炔丙基苄胺盐酸盐
N-甲基-N-丙炔基苄胺 盐酸盐
巴吉林盐酸盐,丙炔甲基苄胺,巴吉林
N-甲基-N-2-丙炔基苄胺 盐酸盐
英文别名
NSC 43798
pargyline hcl
Parguline HCL
pargylinechloride
PARGYLINE HYDROCHLOR
PARGYLINE HYDROCHLORIDE
Parglycine hydrochloride
Pargylamine hydrochloride
Pargyline Hydrochloride (200 mg)
PARGYLINE HYDROCHLORIDE USP/EP/BP
所属类别
原料药:抗高血压病药

物理化学性质

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
形态结晶固体
颜色Crystals from EtOH/Et2O
Merck13,7110
BRN3699487
InChIKeyBCXCABRDBBWWGY-UHFFFAOYSA-N
CAS 数据库306-07-0

安全数据

危险性符号(GHS)
GHS06
警示词危险
危险性描述H301
防范说明P301+P310
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 Germany3
RTECS号DP6650000
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

应用领域

用途1
具有明显的降压作用,单胺氧化酶(MAO-B)选择性抑制剂。

常见问题列表

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
TargetValue
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.

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