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富马酸喹硫平 /Quetiapine hemifumarate {[allProObj[0].p_purity_real_show]}

货号：A742781 同义名： Quetiapine (hemifumarate);ICI-204636 fumarate Ambeed 开学季，买赠积分，赢豪礼

Quetiapine Fumarate is a second-generation antipsychotic with affinity for D2, 5-HT2A, H1, alpha 1 and 5-HT1A receptors, used as an atypical antipsychotic for the treatment of schizophrenia, bipolar disorder, and major depressive disorder.

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Quetiapine hemifumarate 化学结构 CAS号：111974-72-2
Quetiapine hemifumarate 化学结构
CAS号：111974-72-2
Quetiapine hemifumarate 3D分子结构
CAS号：111974-72-2
Quetiapine hemifumarate 化学结构 CAS号：111974-72-2
Quetiapine hemifumarate 3D分子结构 CAS号：111974-72-2
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Quetiapine hemifumarate 纯度/质量文件 产品仅供科研

货号：A742781 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 5-HT ↓ 5-HT1 ↓ 5-HT2 ↓ 5-HT3 ↓ 5-HT5 ↓ 5-HT6 ↓ 5-HT7 ↓ 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

 		{[allProObj[0].p_purity_real_show]}
Lamotrigine +

5-HT (rat brain synaptosomes), IC50: 474 μM

5-HT (human platelets), IC50: 240 μM

 		{[allProObj[0].p_purity_real_show]}
Venlafaxine ✔ {[allProObj[0].p_purity_real_show]}
Fluvoxamine maleate ✔ {[allProObj[0].p_purity_real_show]}
Iloperidone ✔ {[allProObj[0].p_purity_real_show]}
Ziprasidone HCl ✔ {[allProObj[0].p_purity_real_show]}
Atomoxetine HCI +

5-HT, Ki: 77 nM

 		{[allProObj[0].p_purity_real_show]}
Dapoxetine HCl ✔ {[allProObj[0].p_purity_real_show]}
Trazodone ✔ {[allProObj[0].p_purity_real_show]}
Clomipramine HCl ✔ {[allProObj[0].p_purity_real_show]}
Mirtazapine ✔ {[allProObj[0].p_purity_real_show]}
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

 		{[allProObj[0].p_purity_real_show]}
Duloxetine ✔ {[allProObj[0].p_purity_real_show]}
Sertraline HCl ++

5-HT, Ki: 13 nM

 		{[allProObj[0].p_purity_real_show]}
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

 		{[allProObj[0].p_purity_real_show]}
Latrepirdine 2HCl ✔ GluR {[allProObj[0].p_purity_real_show]}
Fluoxetine HCl ✔ {[allProObj[0].p_purity_real_show]}
Paroxetine hydrochloride ✔ AChR {[allProObj[0].p_purity_real_show]}
BMY 7378 ++

5-HT1A, pIC50: 6.4

5-HT1D, pIC50: 5.9

 		+

5-HT2, pIC50: 5.5

 		{[allProObj[0].p_purity_real_show]}
Flibanserin +++

5-HT1A, Ki: 1 nM

 		+

5-HT2A, Ki: 49 nM

 		{[allProObj[0].p_purity_real_show]}
LY310762 +

5-HT1D, Ki: 249 nM

 		{[allProObj[0].p_purity_real_show]}
Cyclobenzaprine HCI ✔ {[allProObj[0].p_purity_real_show]}
Blonanserin +++

5-HT2, Ki: 3.98 nM

 		{[allProObj[0].p_purity_real_show]}
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

 		{[allProObj[0].p_purity_real_show]}
Olanzapine ✔ {[allProObj[0].p_purity_real_show]}
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

 		{[allProObj[0].p_purity_real_show]}
Ketanserin +++

5-HT2C (Human), Ki: 2.5 nM

5-HT2C (Rat), Ki: 50 nM

 		{[allProObj[0].p_purity_real_show]}
Loxapine succinate ++

5-HT2 (bovine), Ki: 6.6 nM

5-HT2 (human), Ki: 6.8 nM

 		{[allProObj[0].p_purity_real_show]}
Agomelatine ✔ {[allProObj[0].p_purity_real_show]}
Clozapine ✔ {[allProObj[0].p_purity_real_show]}
Amitriptyline +

5-HT2, Ki: 235 nM

 		SERT {[allProObj[0].p_purity_real_show]}
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

 		{[allProObj[0].p_purity_real_show]}
RS-127445 ++++

5-HT2B, pIC50: 10.4

5-HT2B, pKi: 9.5

 		{[allProObj[0].p_purity_real_show]}
Sarpogrelate HCl ++++

5-HT2A, Kd: 2.1 nM

5-HT2C, Kd: 1.1 nM

 		{[allProObj[0].p_purity_real_show]}
Tropisetron ✔ {[allProObj[0].p_purity_real_show]}
Palonosetron ✔ {[allProObj[0].p_purity_real_show]}
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

 		{[allProObj[0].p_purity_real_show]}
Ondansetron ✔ {[allProObj[0].p_purity_real_show]}
Granisetron ✔ {[allProObj[0].p_purity_real_show]}
Alosetron HCl ✔ {[allProObj[0].p_purity_real_show]}
Ondansetron hydrochloride dihydrate ✔ {[allProObj[0].p_purity_real_show]}
VUF10166 ++++

5-HT3AB, Ki: 22 nM

5-HT3A, Ki: 0.04 nM

 		{[allProObj[0].p_purity_real_show]}
Azasetron hydrochloride ++++

5-HT3, IC50: 0.33 nM

 		{[allProObj[0].p_purity_real_show]}
Asenapine maleate +++

5-HT1A, pKi: 8.6

5-HT1B, pKi: 8.4

 		++++

5-HT2C, pKi: 10.46

5-HT2A, pKi: 9.75

 		+++

5-HT5A, pKi: 8.84

 		++++

5-HT6, pKi: 9.6

 		++++

5-HT7, pKi: 9.94

 		{[allProObj[0].p_purity_real_show]}
Risperidone ++

5-HT1D, Ki: 84.6 nM

5-HT1B, Ki: 14.9 nM

 		++++

5-HT2C, Ki: 12 nM

5-HT2A, Ki: 61.9 nM

 		+

5-HT5A, Ki: 206 nM

 		++

5-HT7, Ki: 6.6 nM

 		{[allProObj[0].p_purity_real_show]}
SB 271046 HCl +++

5-HT6, pKi: 8.92

 		{[allProObj[0].p_purity_real_show]}
Intepirdine ++++

5-HT6, pKi: 9.63

 		{[allProObj[0].p_purity_real_show]}
SB-269970 HCl ++

5-HT7, pKi: 8.3

 		{[allProObj[0].p_purity_real_show]}
BRL 15572 ++

5-HT1D, pKi: 6

5-HT1B, pKi: 6.1

 		++

5-HT2B, pKi: 6.2

5-HT2A, pKi: 6.6

 		+

5-HT6, pKi: 5.9

 		+

5-HT7, pKi: 6.3

 		{[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 D1 receptor ↓ D2 receptor ↓ D3 receptor ↓ D4 receptor ↓ D5 receptor ↓ DAT ↓ Dopamine receptor ↓ 其他靶点 纯度
Penfluridol +

Dopamine receptor, Ki: 1.6 μM

 		{[allProObj[0].p_purity_real_show]}
Ansofaxine HCl ++

Dopamine receptor, IC50: 491 nM

 		{[allProObj[0].p_purity_real_show]}
Tetrahydroberberine,THB +

D2 receptor, pKi: 6.08

 		{[allProObj[0].p_purity_real_show]}
Prochlorperazine Maleate ✔ {[allProObj[0].p_purity_real_show]}
Olanzapine ✔ {[allProObj[0].p_purity_real_show]}
Trifluoperazine ++++

Dopamine D2 receptor, IC50: 1.1 nM

 		{[allProObj[0].p_purity_real_show]}
Ropinirole hydrochloride ++

D2 receptor, Ki: 29 nM

 		{[allProObj[0].p_purity_real_show]}
Lurasidone ++++

D2 receptor, Ki: 1 nM

 		{[allProObj[0].p_purity_real_show]}
Levosulpiride ✔ {[allProObj[0].p_purity_real_show]}
Pridopidine ✔ {[allProObj[0].p_purity_real_show]}
Metoclopramide ✔ ✔ {[allProObj[0].p_purity_real_show]}
Molindone HCl ✔ {[allProObj[0].p_purity_real_show]}
Sulpiride ✔ {[allProObj[0].p_purity_real_show]}
Perospirone ++++

D2 receptor, Ki: 1.4 nM

 		{[allProObj[0].p_purity_real_show]}
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

 		{[allProObj[0].p_purity_real_show]}
Phenothiazine ✔ {[allProObj[0].p_purity_real_show]}
Pimozide +

Dopamine D1 receptor, Ki: 6600 nM

 		+++

Dopamine D2 receptor, Ki: 3.0 nM

 		++++

Dopamine D3 receptor, Ki: 0.83 nM

 		{[allProObj[0].p_purity_real_show]}
Rotundine ++

D1 receptor, IC50: 166 nM

 		+

D2 receptor, IC50: 1.47 μM

 		+

D3 receptor, IC50: 3.25 μM

 		{[allProObj[0].p_purity_real_show]}
Domperidone ✔ {[allProObj[0].p_purity_real_show]}
ONC206 ✔ {[allProObj[0].p_purity_real_show]}
Pimethixene maleate ++

Dopamine D1 Receptor, pKi: 6.37

 		+++

Dopamine D2 Receptor, pKi: 8.19

 		++

Dopamine D4.4 Receptor, pKi: 7.54

 		{[allProObj[0].p_purity_real_show]}
Loxapine succinate ++

D2 receptor (Human), Ki: 62 nM

D1 receptor (human), Ki: 26 nM

 		++

D2 receptor (bovine), Ki: 26 nM

D2 receptor (human), Ki: 24 nM

 		+++

D4 receptor (human), Ki: 7.5 nM

 		{[allProObj[0].p_purity_real_show]}
Chlorprothixene +++

D1 receptor, Ki: 18 nM

 		+++

D2 receptor, Ki: 2.96 nM

 		+++

D3 receptor, Ki: 4.56 nM

 		+++

D5 receptor, Ki: 9 nM

 		{[allProObj[0].p_purity_real_show]}
SCH-23390 HCl ++++

D1 dopamine receptor, Ki: 0.2 nM

 		++++

D5 dopamine receptor, Ki: 0.3 nM

 		{[allProObj[0].p_purity_real_show]}
MPP+ iodide ✔ {[allProObj[0].p_purity_real_show]}
σ1 Receptor antagonist-1 +

DAT, pKi: 5.8

 		{[allProObj[0].p_purity_real_show]}
Benztropine mesylate ++

DAT, IC50: 118 nM

 		{[allProObj[0].p_purity_real_show]}
Azaperone ✔ {[allProObj[0].p_purity_real_show]}
Ziprasidone HCl ✔ {[allProObj[0].p_purity_real_show]}
Paliperidone ✔ {[allProObj[0].p_purity_real_show]}
Alizapride HCl ✔ {[allProObj[0].p_purity_real_show]}
Amisulpride ✔ {[allProObj[0].p_purity_real_show]}
Quetiapine hemifumarate ✔ Adrenergic Receptor {[allProObj[0].p_purity_real_show]}
Clozapine N-oxide ✔ {[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Quetiapine hemifumarate 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].

Quetiapine hemifumarate 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 <<

Quetiapine hemifumarate 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

Quetiapine hemifumarate 实验方案

计算器
存储液制备 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

Quetiapine hemifumarate 技术信息

CAS号111974-72-2
分子式C46H54N6O8S2
分子量 883.086
别名 Quetiapine (hemifumarate);ICI-204636 fumarate;ICI 204636;Quetiapine fumarate
运输蓝冰
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

Tags: Quetiapine hemifumarate | 111974-72-2 | 5-HT Agonist/D2 Antagonist | GPCR/G Protein | Neuronal Signaling | 5-HT Receptor | Dopamine Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Quetiapine hemifumarate 纯度/质量文件 | Quetiapine hemifumarate 亚型比较 | Quetiapine hemifumarate 生物活性 | Quetiapine hemifumarate 临床数据 | Quetiapine hemifumarate 参考文献 | Quetiapine hemifumarate 实验方案 | Quetiapine hemifumarate 技术信息

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