产品说明书

Sertraline HCl

Print
Chemical Structure| 79559-97-0 同义名 : Sertraline (hydrochloride);CP-51974-1 HCl;CP 51,974-1;Sertraline hydrochloride
CAS号 : 79559-97-0
货号 : A217943
分子式 : C17H18Cl3N
纯度 : 98%
分子量 : 342.69
MDL号 : MFCD00895772
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(145.9 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: 2.5 mg/mL(7.3 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
靶点

  • 5-HT

    5-HT, Ki:13 nM
描述 Sertraline hydrochloride is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class[3]. Sertraline (10 mg/kg) is shown to produce the optimal anti-depression effectsin chronic unpredictable mild stress (CUMS)-exposed mice[4]. Male and female Wistar adult rats were subjected to the FST and sertraline was used as an antidepressant in two doses (10 mg/kg and 40 mg/kg, 3 injections in 24 h). Sertraline at both doses enhanced swimming in both sexes, but females appeared more responsive to lower sertraline doses regarding immobility levels[5]. Milnacipran (30 mg/kg) and sertraline (50 mg/kg) produced statistically significant analgesic effect compared to their control values after acute and chronic application in tail-flick test. The analgesic effects of both milnacipran (30 mg/kg) and sertraline (50 mg/kg) in the presence of L-NAME (10 mg/kg), naloxone (5 mg/kg), ondansetron (0.1 mg/kg) and prazosin (1 mg/kg) were inhibited in tail-flick test[6]. Sertraline dose-dependently increased the locomotor stimulating effect of amphetamine. At the highest dose, 20 mg/kg sertraline had a biphasic effect on amphetamine-induced hyperactivity, producing an initial reduction in amphetamine-induced hyperactivity that was later followed by an augmentation of amphetamine-induced hyperactivity in the last hour of the 3-h test[7].
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
NCT01302080 - Active, not recruiting October 1, 2020 -
NCT00508859 Depression Phase 4 Completed - Canada, British Columbia ... 展开 >> UBC Vancouver, British Columbia, Canada Canada, Nova Scotia Dalhousie University Halifax, Nova Scotia, Canada, B3K 6R8 收起 <<
NCT01703039 Major Depressive Disorder Phase 2 Recruiting September 2019 United States, Massachusetts ... 展开 >> Brigham and Women's Hospital Recruiting Boston, Massachusetts, United States, 02115 Contact: Molly O'Reilly, MA       RAPID@PARTNERS.ORG    Contact: David Wolfe, MD       DWOLFE@PARTNERS.ORG    Principal Investigator: David J Wolfe, MD, MPH 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.92mL

0.58mL

0.29mL

14.59mL

2.92mL

1.46mL

29.18mL

5.84mL

2.92mL
参考文献

[1]Murdoch D, McTavish D. Sertraline. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in depression and obsessive-compulsive disorder. Drugs. 1992 Oct;44(4):604-24.

[2]Koe BK. Preclinical pharmacology of sertraline: a potent and specific inhibitor of serotonin reuptake. J Clin Psychiatry. 1990 Dec;51 Suppl B:13-7.

[3]Murdoch D, McTavish D. Sertraline. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in depression and obsessive-compulsive disorder. Drugs. 1992 Oct;44(4):604-24

[4]Xu X, Zeng XY, Cui YX, Li YB, Cheng JH, Zhao XD, Xu GH, Ma J, Piao HN, Jin X, Piao LX. Antidepressive Effect of Arctiin by Attenuating Neuroinflammation via HMGB1/TLR4- and TNF-α/TNFR1-Mediated NF-κB Activation. ACS Chem Neurosci. 2020 Aug 5;11(15):2214-2230

[5]Kokras N, Antoniou K, Mikail HG, Kafetzopoulos V, Papadopoulou-Daifoti Z, Dalla C. Forced swim test: What about females? Neuropharmacology. 2015 Dec;99:408-21

[6]Kesim M, Yanik MN, Kadioglu M, Pepeoglu D, Erkoseoglu I, Kalyoncu NI, Yaris E. The evaluation of analgesic effects of milnacipran and sertraline in tail-flick test. Bratisl Lek Listy. 2014;115(1):3-6

[7]Sills TL, Greenshaw AJ, Baker GB, Fletcher PJ. The potentiating effect of sertraline and fluoxetine on amphetamine-induced locomotor activity is not mediated by serotonin. Psychopharmacology (Berl). 1999 Apr;143(4):426-32