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产品描述：基本信息 产品编号：P10868 产品名称：Paroxetine hydrochloride CAS: 78246-49-8   储存条件 粉末 室温 四年     分子式： C19H21ClFNO3 溶于液体 -80℃ 两年 分子量 365.83 -20℃ 一个月 化学名：  (3S,4R)-3-((Benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine hydrochloride   Solubility (25°C)   体外 DMSO 73mg/mL (199.54mM) Ethanol 35mg/mL (95.67mM) Water 1mg/mL (2.73mM) 体内 现配现用   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.7335mL 13.6676mL 27.3351mL 5mM 0.5467mL 2.7335mL 5.4670mL 10mM 0.2734mL 1.3668mL 2.7335mL 50mM 0.0547mL 0.2734mL 0.5467mL   生物活性 产品描述 一种高效的五羟色胺再摄取 (serotonin-reuptake) 抑制剂，能抑制 GRK2 活性，IC50 值为 14?μM。Paroxetine hydrochloride 可用于抑郁症的研究。 靶点/IC50 GRK2 IC50: 14μM   体外研究 Paroxetine (1μM and 10μM) distinctly restrains T cell migration induced by CX3CL1 through inhibiting GRK2. Paroxetine inhibits GRK2 induced activation of ERK. Paroxetine (10μM) reduces pro-inflammatory cytokines in LPS-stimulated BV2 cells. Paroxetine (0-5μM) 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 (5μM) 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 (20mg/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.   推荐实验方法(仅供参考) 细胞实验：   Cell Assay Cell viability is determined by the tetrazolium salt 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay. BV2 and primary microglial cells are initially seeded into 96-well plates at a density of 1×104 cells/well and 5×104 cells/well, respectively. Following treatment, MTT (5 mg/mL in PBS) is added to each well and incubated at 37°C for four hours. The resulting formazan crystals are dissolved in dimethylsulfoxide (DMSO). The optical density is measured at 570nm, and results are expressed as a percentage of surviving cells compared with the control.   动物实验:   Animal Administration Animals are divided into two main groups: 1) pre-emptive and 2) post-injury group. Each main group is divided into three different subgroups: I) CCI vehicle-treated group, II) sham group, and III) CCI paroxetine-treated group. Vehicle is injected i.p. to CCI and sham-operated animals. In the pre-emptive study, paroxetine (10mg/kg) is injected 1 h before surgery and continued daily until day 14 post surgery. In the post-injury group, paroxetine (10mg/kg) is administered at day 7 post injury and continued daily until day 14. All behavioral tests are recorded on day 0 (control day) before surgery and on days 1, 3, 5, 7, 10, and 14 post-nerve injury.
保存条件：室温

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