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Quetiapine hemifumarate

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Chemical Structure| 111974-72-2 同义名 : Quetiapine (hemifumarate);ICI-204636 fumarate;ICI 204636;Quetiapine fumarate
CAS号 : 111974-72-2
货号 : A742781
分子式 : C46H54N6O8S2
纯度 : 98%
分子量 : 883.086
MDL号 : MFCD03423782
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: 50 mg/mL(56.62 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: 1 mg/mL(1.13 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • Dopamine receptor
描述 Quetiapine fumarate, as a 5-HT receptors agonist and a dopamine receptor antagonist, has antidepressant and anxiolytic effects[3]. Quetiapine resulted in significantly greater cognitive impairment, higher rates of falls and injury and increased mortality in patients with parkinsonism, but not in patients with dementia. Compared with risperidone and olanzapine, quetiapine had significantly lower risk of mortality, reduced rate of cerebrovascular events, increased rate of falls and injury and less metabolic disorders compared with olanzapine, but higher metabolic disorders compared with risperidone[4]. Quetiapine monotherapy is effective for acute bipolar depression and the prevention of mania/hypomania switching. Its common adverse effects are extrapyramidal side effects, sedation, somnolence, dizziness, fatigue, constipation, dry mouth, increased appetite, and weight gain[5]. Based on this meta-analysis, quetiapine-XR (extended-release) is efficacious in the treatment of GAD (generalized anxiety disorder) in adult patients. Despite its low acceptability and tolerability, the use of 50-150 mg/day quetiapine-XR for adult GAD patients may be considered as an alternative treatment[6].
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
NCT00393978 Bipolar Disorder ... 展开 >> Cannabis-Related Disorder 收起 << Phase 4 Completed - United States, Ohio ... 展开 >> University of Cincinnati Medical Center Cincinnati, Ohio, United States, 45219-0516 收起 <<
NCT00393978 - Completed - -
NCT00306540 Post-Traumatic Stress Disorder Phase 3 Completed - Australia, Queensland ... 展开 >> Research Site Brisbane, Queensland, Australia Australia, South Australia Research Site Adelaide, South Australia, Australia Australia, Victoria Research Site Melbourne, Victoria, Australia 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.13mL

0.23mL

0.11mL

5.66mL

1.13mL

0.57mL

11.32mL

2.26mL

1.13mL
参考文献

[1]Xu H, Chen Z, et al. Synergetic effects of quetiapine and venlafaxine in preventing the chronic restraint stress-induced decrease in cell proliferation and BDNF expression in rat hippocampus. Hippocampus. 2006;16(6):551-9.

[2]Nemeroff CB, Kinkead B, et al. Quetiapine: preclinical studies, pharmacokinetics, drug interactions, and dosing. J Clin Psychiatry. 2002;63 Suppl 13:5-11.

[3]Cross AJ, Widzowski D, Maciag C, et al. Quetiapine and its metabolite norquetiapine: translation from in vitro pharmacology to in vivo efficacy in rodent models. Br J Pharmacol. 2016;173(1):155‐166

[4]El-Saifi N, Moyle W, Jones C, Tuffaha H. Quetiapine safety in older adults: a systematic literature review. J Clin Pharm Ther. 2016;41(1):7‐18

[5]Suttajit S, Srisurapanont M, Maneeton N, Maneeton B. Quetiapine for acute bipolar depression: a systematic review and meta-analysis. Drug Des Devel Ther. 2014;8:827‐838. Published 2014 Jun 25

[6]Maneeton N, Maneeton B, Woottiluk P, et al. Quetiapine monotherapy in acute treatment of generalized anxiety disorder: a systematic review and meta-analysis of randomized controlled trials. Drug Des Devel Ther. 2016;10:259‐276. Published 2016 Jan 12