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306-07-0

中文名稱 巴吉林,優(yōu)降寧
英文名稱 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 2024/11/05 14:42:42
306-07-0 結(jié)構(gòu)式 306-07-0 結(jié)構(gòu)式

基本信息

中文別名
鹽酸帕吉林
丙炔甲基芐胺
巴吉林鹽酸鹽
巴吉林,優(yōu)降寧
優(yōu)降寧 鹽酸鹽
鹽酸帕吉林 標(biāo)準(zhǔn)品
N-甲基-N-炔丙基芐胺鹽酸鹽
N-甲基-N-丙炔基芐胺 鹽酸鹽
巴吉林鹽酸鹽,丙炔甲基芐胺,巴吉林
N-甲基-N-2-丙炔基芐胺 鹽酸鹽
英文別名
NSC 43798
pargyline hcl
Parguline HCL
pargylinechloride
PARGYLINE HYDROCHLOR
PARGYLINE HYDROCHLORIDE
Parglycine hydrochloride
Pargylamine hydrochloride
Pargyline Hydrochloride (200 mg)
PARGYLINE HYDROCHLORIDE USP/EP/BP
所屬類別
原料藥:抗高血壓病藥

物理化學(xué)性質(zhì)

熔點(diǎn)160-163 °C(lit.)
儲(chǔ)存條件−20°C
溶解度≥33.55 mg/mL in EtOH; ≥51.6 mg/mL in H2O; ≥7.55 mg/mL in DMSO
形態(tài)結(jié)晶固體
顏色Crystals from EtOH/Et2O
Merck13,7110
BRN3699487
InChIKeyBCXCABRDBBWWGY-UHFFFAOYSA-N
CAS 數(shù)據(jù)庫(kù)306-07-0

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS06
警示詞危險(xiǎn)
危險(xiǎn)性描述H301
防范說(shuō)明P301+P310
危險(xiǎn)品標(biāo)志Xn
危險(xiǎn)類別碼22
安全說(shuō)明22-24/25
危險(xiǎn)品運(yùn)輸編號(hào)UN 2811 6.1/PG 3
WGK Germany3
RTECS號(hào)DP6650000
危險(xiǎn)等級(jí)6.1(b)
包裝類別III
海關(guān)編碼2921199990
毒性LD50 orl-rat: 250 mg/kg 27ZQAG -,401,72

應(yīng)用領(lǐng)域

用途1
具有明顯的降壓作用,單胺氧化酶(MAO-B)選擇性抑制劑。

常見(jiàn)問(wèn)題列表

生物活性
Pargyline hydrochloride 是一種不可逆的單胺氧化酶 (MAO) 抑制劑,對(duì) MAO-A 和 MAO-B 的 Ki 分別為 13 μM 和 0.5 μM。Pargyline hydrochloride 具有降壓和抗癌活性。
靶點(diǎn)
TargetValue
MAO-B
(Cell-free assay)
0.5 μM(Ki)
MAO-A
(Cell-free assay)
13 μM(Ki)
體外研究

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.
體內(nèi)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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