盐酸帕罗西汀半水合物

中文名称:

盐酸帕罗西汀

中文同义词:

D4-盐酸帕罗西汀;半水帕罗西汀;(-)-反式-4R-(4-氟苯基)-3S-{[3,4-(亚甲二氧基)苯氧基]甲基}-哌啶盐酸盐半水合物;盐酸帕罗西汀半水合物;盐酸帕罗西汀半水合物, 选择性5-羟色胺重吸收抑制剂 (SSRI);(-)-(3S,4R)-PAROXETINE HYDROCHLORIDE HEMIHYDRATE;(办证)盐酸帕罗西汀PAROXETINE HYDROCHLORIDE HEMIHYDRAT

英文名称:

PAROXETINE-D4 HCL

英文同义词:

Piperidine, 3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)-, hydrochloride, hydrate (2:1), (3S,4R)- (9CI);1,3-benzodioxol-5-yl-[4-(4-fluorophenyl)-3-piperidinyl]methanol hydrochloride;PAROXETINE-D4 HCL kf-yuwen(at)kf-chem.com;Piperidine, 3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)-, hydrochloride, hydrate (2:1), (3S-trans)-;Paroxetine Hydrochloride (350 mg);Paroxetine Hydrochloride (350 mg)G0D0030.972mg/mg(ai);Paroxetine-D4 hydrochloride;PAROXETINE-D4 HCL

CAS号:

110429-35-1

分子式:

C19H17ClD4FNO3

分子量:

369.85

EINECS号:

相关类别:

神经信号;对照品;化工中间体;原料药;医用原料;Active Pharmaceutical Ingredients;Cnbio;Serotonin

Mol文件:

110429-35-1.mol

熔点 

121-131 C

溶解度 

Slightly soluble in water, freely soluble in methanol, sparingly soluble in ethanol (96 per cent) and in methylene chloride.

形态

powder

颜色

white

最大波长(λmax)

292nm(H2O)(lit.)

Merck 

14,7043

CAS 数据库

110429-35-1

生物活性

Paroxetine hydrochloride hemihydrate 是一种抗抑郁药，为高效的五羟色胺再摄取抑制剂，能抑制 GRK2 活性，IC50 值为 14 μM。

靶点

IC50: 14 μM (GRK2)

体外研究

Paroxetine (1 μM and 10 μM) distinctly restrains T cell migration induced by CX3CL1 through inhibiting GRK2. Paroxetine inhibits GRK2 induced activation of ERK. Paroxetine (10 μM) reduces pro-inflammatory cytokines in LPS-stimulated BV2 cells. Paroxetine (0-5 μM) leads to a dose-dependent inhibition on LPS-induced production of TNF-α and IL-1β in BV2 cells. Paroxetine also inhibits lipopolysaccharide (LPS)-induced nitric oxide (NO) production and inducible nitric oxide synthase (iNOS) expression in BV2 cells. Paroxetine (5 μM) blocks LPS-induced JNK activation and attenuates baseline ERK1/2 activity in BV2 cells. Paroxetine relieves microglia-mediated neurotoxicity, and suppresses LPS-stimulated pro-inflammatory cytokines and NO in primary microglial cells.

体内研究

Paroxetine treatment obviously attenuates the symptoms of CIA rats. Paroxetine treatment clearly prevents the histological damage of joints and alleviates T cells infiltration into synovial tissue. Paroxetine reveals a strong effect on inhibiting CX3CL1 production in synovial tissues. Paroxetine (20 mg/kg/day) reduces the myocyte cross-sectional area in rat and ROS formation in the remote myocardium. Paroxetine reduces the susceptibility to ventricular tachycardia. Paroxetine treatment following MI decreases LV remodeling and susceptibility to arrhythmias, probably by reducing ROS formation. In CCI paroxetine-treated group, paroxetine (10 mg/kg, i.p.) produces hyperalgesia at days 7 and 10 (P<0.01), but a decrease in pain behavior is seen at day 14. Moreover, paroxetine (10 mg/kg) significantly attenuates tactile hypersensitivity when compared to CCI vehicle-treated group.

危险品标志 

F,C,Xn

危险类别码 

11-34-36/37/38-22

安全说明 

16-26-36/37/39-45-36

危险品运输编号 

UN 3077 9 / PGIII

WGK Germany 

3

RTECS号

TM4569320

HazardClass 

IRRITANT

海关编码 

29349990