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盐酸帕罗西汀

盐酸帕罗西汀用途

Paroxetine hydrochloride 是一种抗抑郁药,为高效的五羟色胺再摄取抑制剂,能抑制 GRK2 活性,IC50 值为 14 μM。

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盐酸帕罗西汀名称

[ CAS 号 ]:
78246-49-8

[ 中文名 ]:
盐酸帕罗西汀

[ 英文名 ]:
Paroxetine HCl

[中文别名 ]:

[英文别名 ]:

MFCD00797405
Paroxetine HCl
Paroxetine Hydrochloride

盐酸帕罗西汀生物活性

[ 描述 ]:

Paroxetine hydrochloride 是一种抗抑郁药,为高效的五羟色胺再摄取抑制剂,能抑制 GRK2 活性,IC50 值为 14 μM。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

信号通路 >> 神经信号通路 >> 5-羟色胺转运蛋白

研究领域 >> 神经疾病

[ 靶点 ]

IC50: 14 μM (GRK2)[3]

[体外研究]

帕罗西汀(1μM和10μM)通过抑制GRK2明显抑制CX3CL1诱导的T细胞迁移。帕罗西汀抑制GRK2诱导的ERK活化[1]。帕罗西汀(10μM)减少LPS刺激的BV2细胞中的促炎细胞因子。帕罗西汀(0-5μM)导致对LPS诱导的BV2细胞中TNF-α和IL-1β产生的剂量依赖性抑制。帕罗西汀还抑制脂多糖(LPS)诱导的一氧化氮(NO)产生和BV2细胞中诱导型一氧化氮合酶(iNOS)的表达。帕罗西汀(5μM)阻断LPS诱导的JNK活化并减弱BV2细胞中的基线ERK1/2活性。帕罗西汀缓解小胶质细胞介导的神经毒性,并抑制原代小胶质细胞中LPS刺激的促炎细胞因子和NO [4]。

[体内研究]

帕罗西汀治疗明显减轻了CIA大鼠的症状。帕罗西汀治疗明确预防关节的组织学损伤并减轻T细胞浸润到滑膜组织中。帕罗西汀显示出对抑制滑膜组织中CX3CL1产生的强烈作用[1]。帕罗西汀(20mg/kg /天)减少大鼠的肌细胞横截面积和远端心肌中的ROS形成。帕罗西汀可降低对室性心动过速的易感性。 MI后的帕罗西汀治疗可能通过减少ROS形成来降低LV重塑和对心律失常的易感性[2]。在CCI帕罗西汀治疗组中,帕罗西汀(10 mg/kg,腹腔注射)在第7天和第10天出现痛觉过敏(P <0.01),但在第14天出现疼痛行为减少。此外,帕罗西汀(10 mg/kg)与CCI载体治疗组相比,显着减弱了触觉超敏反应[5]。

[细胞实验]

通过四唑盐3- [4,5-二甲基噻唑-2-基] -2,5-二苯基四唑溴化物（MTT）测定法测定细胞活力。最初将BV2和原代小胶质细胞以1×10 4个细胞/孔和5×10 4个细胞/孔的密度接种到96孔板中。处理后，将MTT（PBS中5mg / mL）加入各孔中，并在37℃下孵育4小时。将得到的甲crystals晶体溶解在二甲基亚砜（DMSO）中。在570nm处测量光密度，结果表示为与对照相比存活细胞的百分比。

[动物实验]

动物分为两大类：1）先发性和2）损伤后组。每个主要组分为三个不同的亚组：I）CCI载体治疗组，II）假组，和III）CCI帕罗西汀治疗组。将载体ip注射到CCI和假手术动物。在先发制剂研究中，帕罗西汀（10 mg / kg）在手术前1小时注射，并且每天持续至手术后第14天。在损伤后组中，帕罗西汀（10mg / kg）在损伤后第7天给药，并且每天持续至第14天。所有行为测试记录在手术前第0天（对照日）和第1,3,5天。，7,10和14后神经损伤。

[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]. 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.

[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.

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

[5]. 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.

[相关活性小分子]

盐酸帕罗西汀物理化学性质

[ 密度 ]:
1.213 g/cm3

[ 沸点 ]:
451.7ºC at 760 mmHg

[ 熔点 ]:
129-131ºC

[ 分子式 ]:
C₁₉H₂₁ClFNO₃

[ 分子量 ]:
365.826

[ 闪点 ]:
227ºC

[ 精确质量 ]:
365.119385

[ PSA ]:
39.72000

[ LogP ]:
4.45730

[ 外观性状 ]:
白色或近乎于白色结晶粉末

[ 储存条件 ]:
-20°C Freezer

盐酸帕罗西汀毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TM4569320

CHEMICAL NAME :: Piperidine, 3-((1,3-benzodioxol-5-yloxy)methyl)-4-(4-fluorophenyl )-, hydrochloride, (3S-trans)-

CAS REGISTRY NUMBER :: 78246-49-8

LAST UPDATED :: 199509

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C19-H20-F-N-O3.Cl-H

MOLECULAR WEIGHT :: 365.86

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 415 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ASSUA6 Acta Psychiatrica Scandinavica, Supplementum. (Munksgaard International Publishers, POB 2148, DK-1016 Copenhagen K, Denmark) No.160- 1961- Volume(issue)/page/year: 350,31,1989

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 30 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ASSUA6 Acta Psychiatrica Scandinavica, Supplementum. (Munksgaard International Publishers, POB 2148, DK-1016 Copenhagen K, Denmark) No.160- 1961- Volume(issue)/page/year: 350,31,1989

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 378 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ASSUA6 Acta Psychiatrica Scandinavica, Supplementum. (Munksgaard International Publishers, POB 2148, DK-1016 Copenhagen K, Denmark) No.160- 1961- Volume(issue)/page/year: 350,31,1989

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 42 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ASSUA6 Acta Psychiatrica Scandinavica, Supplementum. (Munksgaard International Publishers, POB 2148, DK-1016 Copenhagen K, Denmark) No.160- 1961- Volume(issue)/page/year: 350,31,1989

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盐酸帕罗西汀安全信息

[ 危险品运输编码 ]:
UN 3249

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2934999090

盐酸帕罗西汀海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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