盐酸帕罗西汀 T1636

Product Introduction
Bioactivity


英文名: Paroxetine hydrochloride

描述: Paroxetine hydrochloride (Paroxetine HCl) 是一种血清素摄取抑制剂，能抑制 GRK2 活性，IC50值为 14 μM。它可研究抑郁症。

细胞实验: Paroxetine is dissolved in DMSO. 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 570 nm, and results are expressed as a percentage of surviving cells compared with the control.

体外活性: Paroxetine在ED50 1-3 mg/kg PO）可防止对氯苯丙胺（PCA）在大鼠脑中的5-HT消耗作用,表明体内5-HT摄取受阻.Paroxetine对离体大鼠下丘脑突触体产生剂量相关的[3H] -5-HT摄取抑制（ED50 = 1.9 mg/kg）,对[3H] -l-去甲肾上腺素（NA）摄取影响很小（ED50大于30 mg/kg）.

体内活性: 1-300 μM Paroxetine导致ACSF超融合脑干切片中DRN血清素能神经元放电速率浓度依赖性降低,IC50值为1.4 μM。Paroxetine是地昔帕明羟基化的高度有效的抑制剂,抑制常数（Ki）为2 mM,表明其抑制效力比氟西汀或诺氟西汀更强。Paroxetine在大鼠皮层和体外下丘脑突触中,是一种[3H]-5-羟色胺（5-HT）的有效的（Ki=1.1 nM）和特异性抑制剂。Paroxetine显然通过增加细胞外区室中5-HT的浓度来发挥其抗抑郁活性,由此增强血清素能神经传递。 Paroxetine通过形成代谢物中间体复合物来灭活CYP2D6。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 10 mg/mL (27.33 mM)
Ethanol : 35 mg/mL (95.67 mM)
DMSO : 73 mg/mL (199.54 mM)


关键字: BRL 29060 Hydrochloride | Autophagy | Paroxetine Hydrochloride | BRL 29060 | FG7051 | inhibit | Paroxetine | Paroxetine hydrochloride | BRL29060 Hydrochloride | SLC6A4 | BRL-29060 Hydrochloride | BRL29060 | FG 7051 | Inhibitor | SERT | BRL-29060 | 5-HTT | Serotonin Transporter

相关产品: p-MPPI hydrochloride | Nortriptyline hydrochloride | Rotundine | Alniditan | SB-399885 hydrochloride | Jatrorrhizine chloride | SB 243213 dihydrochloride | AL 34662 | AS19 | Adatanserin

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Inhibitor Library | GPCR Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library

盐酸帕罗西汀 T1636信息由TargetMol中国为您提供，如您想了解更多关于盐酸帕罗西汀 T1636报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途