Paroxetine HCl.|78246-49-8|(盐酸帕罗西汀; BRL29060 hydrochloride; BRL29060A)-陌孚医药/Medlife

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Paroxetine HCl. (Synonyms: 盐酸帕罗西汀; BRL29060 hydrochloride; BRL29060A)

目录号: PC14277 纯度: ≥98%

CAS No. :78246-49-8

商品编号	规格	价格	会员价
PC14277-10mg	10mg	¥392.00	请登录
PC14277-100mg	100mg	¥588.00	请登录
PC14277-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥490.00	请登录

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中文名称	Paroxetine HCl.
中文别名	盐酸帕罗西汀;(-)-反式-4-(4-氟苯基)-3-{[3,4-(亚甲二氧基)苯氧基]甲基}-哌啶盐酸盐;(-)-反-4-(4-氟苯基)-3-[[3,4-(甲二氧基)苯氧基]甲基]-哌啶盐酸盐;(-)-反式-4-(4-氟苯基)-3-{[3,4-(甲二氧基)苯氧基]甲基}-哌啶盐酸盐;(-)-反式-4-(4-氟苯基)-3-{[3,4-(甲二氧基)苯氧基]甲基}-哌啶盐酸盐A;盐酸帕罗克赛;帕罗昔丁;帕罗西汀盐酸盐;赛乐特;盐酸帕罗西丁;盐酸帕罗西汀(无水);盐酸帕罗西汀半水合物 EP标准品;盐酸帕罗西汀标准品(JP)
英文名称	Paroxetine HCl
英文别名	(3S-TRANS)-3-[(1,3-BENZODIOXOL-5-YLOXY)METHYL]-4-(4-FLUOROPHENYL)PIPERIDINE;(3s-trans)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl;piperidine hydrochloride;BRL-29060;FG-7051;PAROXETINE HCL;PAROXETINE HYDROCHLORIDE;PAROXETIN X HCL;(-)TRANS-3-[(1,3-BENZODIOXOL-5-YLOXY) METHYL]-4-(4-FLUOROPHENYL) PAROXETINE HYDROCHLORIDE;(3s,4r)-orid;(3s-trans)-id;3-((1,3-benzodioxol-5-yloxy)methyl)-4-(4-fluorophenyl)-,hydrochloride,(3s-trans)-piperidin;3-((1,3-benzodioxol-5-yloxy)methyl)-4-(4-fluorophenyl)-piperidinhydrochl;3-((1,3-benzodioxol-5-yloxy)methyl)-4-(4-fluorophenyl)-piperidinhydrochlor;brl29060a;brl29060hydrochloride;Paroxetine HCL EP4.5;Paroxeting chlorhydric acid;(-)TRANS-3-[(1,3-BENZODIOXOL-5-YLOXY)METHYL]-4-(4-FLUOROPHENYL)PIPERIDINE HYDROCHLORIDE;Deroxat;(3S-Trans)-3-[(1,3-Benzodioxol-5-Yloxy)Methyl]-4-(4-Fluorophenyl)Piperidine Hydrochloride;Paroxetin HCL;Paroxetine (hydrochloride);Paroxetine Hydrochlo;2H2O;ParoxetineHCl.1;Paxil;Paroxat;Aropax 20;(3S,4R)-3-((Benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine hydrochloride;BRL 29060 hydrochloride;Aropax;Paroxetine hydrochloride [USP];BRL 29060A;SDB 7175;Paroxetine hydrochloride hemihydrate;3I3T11UD2S;Paroxetine hydrochloride hemihydrate (MW = 374.83);S3005;Paxil (TN);C19H21ClFNO3;Piperidine, 3-((1,3-benzodioxol-5-yloxy)methyl)-
Cas No.	78246-49-8
分子式	C₁₉H₂₁ClFNO₃
分子量	365.83
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Paroxetine hydrochloride is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an GRK2 inhibitor with IC₅₀ of 14?μM. Paroxetine hydrochloride can be used for the research of depressive disorder.

性状

Solid

IC50 & Target[1][2]

IC50: 14?μM (GRK2)

体外研究(In Vitro)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Wang Q, et al. Paroxetine alleviates T lymphocyte activation and infiltration to joints of collagen-induced arthritis. Sci Rep. 2017 Mar 28;7:45364. [Information]

[2]. Liu RP, et al. Paroxetine ameliorates lipopolysaccharide-induced microglia activation via differential regulation of MAPK signaling. J Neuroinflammation. 2014 Mar 12;11:47. [Information]

[3]. Lassen TR, et al. Effect of paroxetine on left ventricular remodeling in an in vivo rat model of myocardial infarction. Basic Res Cardiol. 2017 May;112(3):26. [Information]

[4]. Zarei M, et al. Paroxetine attenuates the development and existing pain in a rat model of neurophatic pain. Iran Biomed J. 2014;18(2):94-100. [Information]

[5]. Waldschmidt HV, et al. Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine. J Med Chem. 2017 Apr 13;60(7):3052-3069. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (273.35 mM; Need ultrasonic)

H₂O : 5 mg/mL (13.67 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7335 mL	13.6676 mL	27.3351 mL
5 mM	0.5467 mL	2.7335 mL	5.4670 mL
10 mM	0.2734 mL	1.3668 mL	2.7335 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制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

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.83 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.83 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.83 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
4.

建议依照次序添加每种溶剂： PBS
Solubility: 2.03 mg/mL (5.55 mM); Clear solution; Need ultrasonic

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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