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Paroxetine hydrochloride

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Chemical Structure| 78246-49-8 同义名 : BRL29060 hydrochloride;BRL29060A;Paroxetine (hydrochloride);FG-7051;Paroxetine HCl
CAS号 : 78246-49-8
货号 : A212664
分子式 : C19H21ClFNO3
纯度 : 97%
分子量 : 365.826
MDL号 : MFCD00797405
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 :

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
动物实验配方：
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].
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 - -
实验方案
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
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.