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Paroxetine hydrochloride

SKU: orb1307940

描述

Paroxetine hydrochloride is a selective serotonin reuptake inhibitor (SSRI) used in depression research. It is widely applied in both in vitro binding assays and in vivo behavioral studies to investigate serotonergic neurotransmission and antidepressant mechanisms.

研究领域

Cell Biology, Neuroscience, Pharmacology & Drug Discovery

图片与验证

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关键属性

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CAS 号78246-49-8
MW365.826
纯度99.99% (May vary between batches)
分子式C19H21ClFNO3
SMILESCl.Fc1ccc(cc1)[C@@H]1CCNC[C@H]1COc1ccc2OCOc2c1
靶点Autophagy,GRK,5-HT Receptor,Serotonin Transporter,AChR
溶解性10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.47 mM);Ethanol:35 mg/mL (95.67 mM);H2O:10 mg/mL (27.34 mM);DMSO:45 mg/mL (123.01 mM)

生物活性

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靶点 IC50
GRK2:14 μM
体内
Paroxetine, a highly effective hydroxylated metabolite inhibitor of (dextromethorphan), demonstrates the concentration-dependent reduction in the firing rate of serotonergic neurons within the DRN of super fused brainstem slices at 1-300 μM, with an IC50 value of 1.4 μM. With an inhibition constant (Ki) of 2 mM, Paroxetine's inhibitory capacity surpasses that of fluoxetine or norfluoxetine, indicating its more potent effect. Moreover, in rat cortical and in vitro hypothalamic synapses, Paroxetine acts as a potent and specific inhibitor of [3H]-5-hydroxytryptamine (5-HT), with a Ki of 1.1 nM. Its antidepressant activity is attributed to the increased concentration of 5-HT in the extracellular compartment, thereby enhancing serotonergic neurotransmission. Paroxetine also inactivates CYP2D6 by forming metabolic intermediate complexes.
体外
Paroxetine, at an ED50 of 1-3 mg/kg when administered orally (PO), demonstrates the capability to prevent the depletion of serotonin (5-HT) in rats' brains induced by p-chloroamphetamine (PCA), signifying an inhibition of serotonin uptake in vivo. Additionally, in isolated rat hypothalamic synaptosomes, paroxetine exhibits a dose-dependent inhibition of [3H] - 5-HT uptake with an ED50 of 1.9 mg/kg, while showing minimal effects on the uptake of [3H] - norepinephrine (NA), with an ED50 exceeding 30 mg/kg.
细胞研究
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.

储存与操作

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储存-20°C
有效期12 months from date of receipt.
免责声明For research use only

别名

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BRL 29060, BRL 29060 Hydrochloride, BRL29060, BRL-29060, BRL29060 Hydrochloride, BRL29060 hydrochloride, BRL-29060 Hydrochloride, BRL29060A, Autophagy, 5HTReceptor, 5HT Receptor, 5-HT, 5-HTT, AChR, Paroxetine, Paroxetine HCl, Paroxetine Hydrochloride, Paroxetine hydrochloride, inhibit, Inhibitor, FG 7051, FG7051, FG-7051, GRK2, SLC6A4, Serotonin Transporter, SerotoninTransporter, SERT

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质量保证

质量保证

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our 条款与条件和选购指南.

关键属性

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暂无计算属性。

实验方案信息

可选规格

请在下方选择规格

1 ml x 10 mM (in DMSO)
¥ 910.00
50 mg
¥ 1,040.00
100 mg
¥ 1,300.00
500 mg
¥ 2,600.00
发货Usually dispatched within 5-10 working days
批量询价