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Paroxetine hydrochloride hemihydrate

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Chemical Structure| 110429-35-1 同义名 : 盐酸帕罗西汀半水合物 ;BRL29060 hydrochloride hemihydrate;BRL29060A hemihydrate
CAS号 : 110429-35-1
货号 : A531483
分子式 : C38H44Cl2F2N2O7
纯度 : 97%
分子量 : 749.668
MDL号 : MFCD23843784
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Paroxetine, at concentrations of 1 μM and 10 μM, significantly inhibits T cell migration induced by CX3CL1 by blocking GRK2 activity. This inhibition also extends to GRK2-mediated activation of the ERK signaling pathway[1]. At a concentration of 10 μM, Paroxetine decreases the levels of pro-inflammatory cytokines in LPS-stimulated BV2 microglial cells. Furthermore, Paroxetine (0-5 μM) shows a dose-dependent reduction in the LPS-induced production of TNF-α and IL-1β in these cells. It also curbs the LPS-induced production of nitric oxide (NO) and the expression of inducible nitric oxide synthase (iNOS) in BV2 cells. At 5 μM, Paroxetine inhibits LPS-induced JNK activation and reduces baseline ERK1/2 activity, contributing to its ability to mitigate microglial-mediated neurotoxicity and suppress pro-inflammatory cytokines and NO production in primary microglial cells[4].
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
NCT00031317 Panic Disorder Phase 4 Completed - United States, Maryland ... 展开 >> National Institute of Mental Health (NIMH) Bethesda, Maryland, United States, 20892 收起 <<
NCT00445679 - Completed - -
NCT00403455 PTSD Phase 3 Completed - United States, South Carolina ... 展开 >> Ralph H. Johnson VA Medical Center, Charleston, SC Charleston, South Carolina, United States, 29401-5799 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.33mL

0.27mL

0.13mL

6.67mL

1.33mL

0.67mL

13.34mL

2.67mL

1.33mL

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.

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

[3]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.