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首页 / 抑制剂/激动剂 / 神经信号通路 / SSRIs / Paroxetine HCl/盐酸帕罗西汀

Paroxetine HCl/盐酸帕罗西汀 {[allProObj[0].p_purity_real_show]}

货号：A212664 同义名： BRL29060 hydrochloride; BRL29060A

Paroxetine hydrochloride 是一种选择性 5-HT 再摄取抑制剂（SSRI，IC50 14 μM），常用于抑郁症的研究。

Paroxetine HCl/盐酸帕罗西汀 化学结构 CAS号：78246-49-8
Paroxetine HCl/盐酸帕罗西汀 化学结构
CAS号：78246-49-8
Paroxetine HCl/盐酸帕罗西汀 3D分子结构
CAS号：78246-49-8
Paroxetine HCl/盐酸帕罗西汀 化学结构 CAS号：78246-49-8
Paroxetine HCl/盐酸帕罗西汀 3D分子结构 CAS号：78246-49-8
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Paroxetine HCl/盐酸帕罗西汀 纯度/质量文件 产品仅供科研

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Paroxetine HCl/盐酸帕罗西汀 生物活性

靶点

  • AChR

  • 5-HT
描述 Paroxetine is a potent and selective serotonin reuptake inhibitor (SSRI) with Ki value of 1.1nM for inhibition of 5-HT uptake into rat cortical and hypothalamic synaptosomes in vitro. It exhibited weak affinity for muscarinic receptors (Ki=89nM). Oral administration of paroxetine produced a dose-related inhibition of [3H]-5-HT uptake (ED50=1.9mg/kg) into rat hypothalamic synaptosomes ex vivo[3]. It is currently approved indications for the treatment of depression, obsessive-compulsive disorder, panic disorder and social phobia. And it is also used in the treatment of generalized anxiety disorder, post traumatic stress disorder, premenstrual dysphoric disorder and chronic headache[4].

Paroxetine HCl/盐酸帕罗西汀 细胞实验

Cell Line
Concentration Treated Time Description References
MH7A cells 10 μM 24 h Paroxetine markedly suppressed SAV1 phosphorylation, indicating that it prevents the degradation of SAV1. Acta Pharm Sin B. 2024 Mar;14(3):1222-1240.
Primary mouse lung mast cells (LMCs) 30 µM 30 min To study the inhibitory effect of Paroxetine on IgE-mediated degranulation, results showed that Paroxetine significantly inhibited IgE-mediated degranulation. Front Immunol. 2022 Oct 6;13:1032497.
RBL-2H3 cells 30 µM 30 min To study the inhibitory effect of Paroxetine on FcϵRI-mediated calcium mobilization and degranulation, results showed that Paroxetine significantly inhibited FcϵRI-mediated calcium mobilization and degranulation. Front Immunol. 2022 Oct 6;13:1032497.
Human islets 0.01 –1 μM 48 h To evaluate the effect of Paroxetine on insulin secretion in human islet cells. The results showed that 0.01 and 0.1 μM Paroxetine significantly enhanced glucose-stimulated insulin secretion. Diabetes Obes Metab. 2024 Sep;26(9):3606-3617.
Mouse islets 0.01 –1 μM 48 h To evaluate the effect of Paroxetine on the viability of mouse islet cells. The results showed that 0.01 and 0.1 μM Paroxetine had no significant effect on cell viability, while 1 μM Paroxetine was cytotoxic. Diabetes Obes Metab. 2024 Sep;26(9):3606-3617.
MIN6 β cells 0.01 –1 μM 48 h To evaluate the effect of Paroxetine on the viability of MIN6 β cells and islet cells. The results showed that 0.01 and 0.1 μM Paroxetine had no significant effect on cell viability, while 1 μM Paroxetine was cytotoxic. Diabetes Obes Metab. 2024 Sep;26(9):3606-3617.

Paroxetine HCl/盐酸帕罗西汀 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Rats Collagen-induced arthritis (CIA) model Oral 15 mg/kg Once daily for 14 days Paroxetine significantly improved the clinical manifestations of CIA rats and inhibited the abnormal proliferation of FLSs. Acta Pharm Sin B. 2024 Mar;14(3):1222-1240.
Mice C57BL/6 mice Intravenous injection 5 mg/kg Single injection, lasting 30 minutes To study the inhibitory effect of Paroxetine on IgE-mediated passive cutaneous anaphylaxis, results showed that Paroxetine significantly reduced IgE-mediated vascular permeability. Front Immunol. 2022 Oct 6;13:1032497.
Mice Anxiety model Subcutaneous injection 10 mg/kg Once daily for 12 days, then discontinued for 2 or 5 days To investigate the effect of paroxetine discontinuation on 5-HT function, results showed increased 5-HT metabolism in the hippocampus, enhanced 5-HT neuron activity, and increased anxiety-like behavior on day 2 of discontinuation. Neuropsychopharmacology. 2024 Sep;49(10):1580-1589
Spontaneously hypertensive rats Spontaneously hypertensive rat model Gavage 5 mg/kg Once daily for 12 weeks To study the effect of paroxetine on hypertension-induced cardiac hypertrophy, dysfunction, and fibrosis, results showed that paroxetine treatment significantly ameliorated hypertension-induced cardiac hypertrophy, dysfunction, and fibrosis. J Am Heart Assoc. 2021 Jan 5;10(1):e016364
C57BL/6 mice DSS-induced colitis model Oral 20 mg/kg Once daily for 10 days To evaluate the anti-inflammatory effects of Paroxetine in a DSS-induced colitis model, results showed that Paroxetine alleviated colitis inflammation Front Immunol. 2023 Feb 27;14:1145070
Wistar albino rats Isoproterenol-induced cardiac hypertrophy model Oral gavage 5 mg/kg Once daily for 3 weeks To investigate the cardioprotective effects of Paroxetine on cardiac hypertrophy, results showed that Paroxetine pre-treatment significantly reduced the expression of hypertrophic and fibrotic markers and inflammatory markers. Int J Mol Sci. 2023 Dec 8;24(24):17270

Paroxetine HCl/盐酸帕罗西汀 动物研究

Dose Parrot: 10 mg/kg[3] (p.o.) Rat: 10 mg/kg[4] (i.v.); 0.3 mg/kg - 10 mg/kg[5] (p.o.)
Administration p.o., i.v.

Paroxetine HCl/盐酸帕罗西汀 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02273154 Major Depression Disorder Phase 4 Unknown December 2015 China, Beijing ... 展开 >> Institute of mental health, Peking University Not yet recruiting Beijing, Beijing, China, 100191 Contact: Tianmei Si, PhD.    8610-82801960    si.tian-mei@163.com    Principal Investigator: Tianmei Si, PhD.          China, Henan Henan mental health center Recruiting Xinxiang, Henan, China, 453000 Contact: Luxian Lv, MD.    86-13837320007    lvluxian86@hotmail.com    China, Hubei Wuhan mental health center Recruiting Wuhan, Hubei, China, 430000 Contact: Maosheng Fang, MD.    86-13553013182    fangmaosheng@126.com    China, Jiangsu Nanjing Brain Hospital Recruiting Nanjing, Jiangsu, China, 210000 Contact: Zhijian Yao, PhD.    86-13851580276    zhijianyao@163.com    China, Liaoning Dalian No.7 People's Hospital Recruiting Dalian, Liaoning, China, 116000 Contact: Shoufu Xie, MD.    86-18441168381    shoufuxie@126.com    China, Shanxi Shanxi Dayi Hospital Recruiting Taiyuan, Shanxi, China, 030000 Contact: Hong Yang, MD.    86-13903414208    hongyang1964@163.com 收起 <<
NCT00445679 Depressive Disorder, Major Phase 3 Completed - -
NCT00445679 - Completed - -

Paroxetine HCl/盐酸帕罗西汀 参考文献

[1]Thomas DR, Nelson DR, et al. Biochemical effects of the antidepressant paroxetine, a specific 5-hydroxytryptamine uptake inhibitor. Psychopharmacology (Berl). 1987;93(2):193-200.

[2]Bourin M, Chue P, et al. Paroxetine: a review. CNS Drug Rev. 2001 Spring;7(1):25-47.

[3]Thomas DR, Nelson DR, Johnson AM. Biochemical effects of the antidepressant paroxetine, a specific 5-hydroxytryptamine uptake inhibitor. Psychopharmacology (Berl). 1987;93(2):193-200. doi: 10.1007/BF00179933. PMID: 2962217.

[4]Bourin M, Chue P, Guillon Y. Paroxetine: a review. CNS Drug Rev. 2001 Spring;7(1):25-47. doi: 10.1111/j.1527-3458.2001.tb00189.x. PMID: 11420571; PMCID: PMC6741642.

Paroxetine HCl/盐酸帕罗西汀 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.73mL

0.55mL

0.27mL

13.67mL

2.73mL

1.37mL

27.34mL

5.47mL

2.73mL

Paroxetine HCl/盐酸帕罗西汀 技术信息

CAS号78246-49-8
分子式C19H21ClFNO3
分子量 365.83
SMILES Code FC1=CC=C([C@H]2[C@H](COC3=CC=C(OCO4)C4=C3)CNCC2)C=C1.[H]Cl
MDL No. MFCD00797405
别名 BRL29060 hydrochloride; BRL29060A; Paroxetine (hydrochloride); FG-7051; Paroxetine HCl
运输蓝冰
InChI Key GELRVIPPMNMYGS-RVXRQPKJSA-N
Pubchem ID 62878
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C
溶解方案

DMSO: 105 mg/mL(287.02 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 5 mg/mL(13.67 mM)，配合低频超声助溶

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Paroxetine hydrochloride | BRL29060 hydrochloride;BRL29060A;Paroxetine (hydrochloride);FG-7051;Paroxetine HCl | SSRIs | AmBeed-信号通路专用抑制剂 | Paroxetine HCl/盐酸帕罗西汀 纯度/质量文件 | Paroxetine HCl/盐酸帕罗西汀 生物活性 | Paroxetine HCl/盐酸帕罗西汀 动物研究 | Paroxetine HCl/盐酸帕罗西汀 临床数据 | Paroxetine HCl/盐酸帕罗西汀 参考文献 | Paroxetine HCl/盐酸帕罗西汀 实验方案 | Paroxetine HCl/盐酸帕罗西汀 技术信息

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