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神经信号通路 帕金森与阿尔茨海默症
/ 多巴胺受体 / Droperidol/氟哌啶

Droperidol/氟哌啶 {[allProObj[0].p_purity_real_show]}

货号：A541340 同义名： 氟哌利多 / Dehydrobenzperidol; DHBP

Droperidol是多巴胺2受体的拮抗剂。

Droperidol/氟哌啶 化学结构 CAS号：548-73-2
Droperidol/氟哌啶 化学结构
CAS号：548-73-2
Droperidol/氟哌啶 3D分子结构
CAS号：548-73-2
Droperidol/氟哌啶 化学结构 CAS号：548-73-2
Droperidol/氟哌啶 3D分子结构 CAS号：548-73-2
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Droperidol/氟哌啶 纯度/质量文件 产品仅供科研

货号：A541340 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 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

 		98%
Ansofaxine HCl ++

Dopamine receptor, IC50: 491 nM

 		99%
Tetrahydroberberine +

D2 receptor, pKi: 6.08

 		98+%
Prochlorperazine Maleate ✔ 98% (HPLC)
Olanzapine ✔ 99+%
Trifluoperazine ++++

Dopamine D2 receptor, IC50: 1.1 nM

 		98%
Ropinirole HCl ++

D2 receptor, Ki: 29 nM

 		99%
Lurasidone ++++

D2 receptor, Ki: 1 nM

 		98%
Levosulpiride ✔ 99+%
Pridopidine ✔ 95%
Metoclopramide ✔ ✔ 99+%
Molindone HCl ✔ 99%
Sulpiride ✔ 99+%
Perospirone ++++

D2 receptor, Ki: 1.4 nM

 		99%
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

 		99%
Phenothiazine ✔ 98%
Pimozide +

Dopamine D1 receptor, Ki: 6600 nM

 		+++

Dopamine D2 receptor, Ki: 3.0 nM

 		++++

Dopamine D3 receptor, Ki: 0.83 nM

 		98%
Rotundine ++

D1 receptor, IC50: 166 nM

 		+

D2 receptor, IC50: 1.47 μM

 		+

D3 receptor, IC50: 3.25 μM

 		98%
Domperidone ✔ 99+%
ONC206 ✔ 99%
Pimethixene maleate ++

Dopamine D1 Receptor, pKi: 6.37

 		+++

Dopamine D2 Receptor, pKi: 8.19

 		++

Dopamine D4.4 Receptor, pKi: 7.54

 		97%
Loxapine succinate ++

D1 receptor (human), Ki: 26 nM

D2 receptor (Human), Ki: 62 nM

 		++

D2 receptor (human), Ki: 24 nM

D2 receptor (bovine), Ki: 26 nM

 		+++

D4 receptor (human), Ki: 7.5 nM

 		98%
Chlorprothixene +++

D1 receptor, Ki: 18 nM

 		+++

D2 receptor, Ki: 2.96 nM

 		+++

D3 receptor, Ki: 4.56 nM

 		+++

D5 receptor, Ki: 9 nM

 		99%
SCH-23390 HCl ++++

D1 dopamine receptor, Ki: 0.2 nM

 		++++

D5 dopamine receptor, Ki: 0.3 nM

 		98%
MPP+ iodide ✔ 97%
σ1 Receptor antagonist-1 +

DAT, pKi: 5.8

 		97%
Benztropine mesylate ++

DAT, IC50: 118 nM

 		98%
Azaperone ✔ 98%
Ziprasidone HCl ✔ 98+%
Paliperidone ✔ 98%
Alizapride HCl ✔ 99+%
Amisulpride ✔ 98%
Quetiapine hemifumarate ✔ Adrenergic Receptor 98%
Clozapine N-oxide ✔ 99%
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。

Droperidol/氟哌啶 生物活性

描述 Droperidol, a dopamine-2 receptor antagonist, is a butyrophenone, with anti-emetic, sedative and anti-anxiety properties. Parenteral droperidol is an effective option for the treatment of acute migraine. The minimum effective dose is 2.5 mg given IM or IV (intramuscularly or intravenously ). The most commonly reported adverse effects were extrapyramidal symptoms and sedation[3]. QT prolongation is noted with multiple medication classes, and droperidol increases QT interval in a dose-dependent fashion among susceptible individuals[4]. Midazolam-droperidol combination therapy is superior, in the doses studied, to either droperidol or olanzapine monotherapy for intravenous sedation of the acutely agitated ED (emergency department) patient[5]. Droperidol significantly reduced opioid-induced PONV (postoperative nausea and vomiting) in adults during PCA (patient-controlled analgesia) and had a morphine-sparing effect. Droperidol is generally well tolerated and the incidence of adverse effects is similar to that observed with placebo and the serotonin 5-HT3 receptor antagonists (setrons)[6].

Droperidol/氟哌啶 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
NCT03506789 Postoperative Pain Phase 4 Recruiting June 30, 2020 Denmark ... 展开 >> Gildhøj Privathospital Not yet recruiting Brøndbyvester, Denmark, 2605 Contact: Niels A Pedersen, MD          Bispebjerg Hospital Recruiting Copenhagen, Denmark, 2400 Contact: Troels H Lunn, DMSc          Sjællands Universitetshospital, Køge Not yet recruiting Køge, Denmark, 4600 Contact: Ole Mathiesen, MD, PhD, Assoc Prof.          Næstsved Sygehus Recruiting Næstved, Denmark, 4700 Contact: Kasper S Gasbjerg, MD          Odense Universitetshospital Not yet recruiting Odense, Denmark, 5000 Contact: Søren Overgaard, DMSc 收起 <<
NCT03618082 Immediate Severe Postoperative... 展开 >> Pain Perioperative Hemodynamic 收起 << Phase 3 Not yet recruiting March 31, 2021 France ... 展开 >> CHU Clermont-Ferrand Not yet recruiting Clermont-Ferrand, Auvergne, France, 63003 Contact: Lise LACLAUTRE    04 73 75 49 63    drci@chu-clermontferrand.fr    Principal Investigator: Jean-Etienne BAZIN          Sub-Investigator: Bernard ALLAOUICHE          Sub-Investigator: Emmanuel FUTIER          Sub-Investigator: Lionel BOUVET          Sub-Investigator: Régis FUZIER          Sub-Investigator: Elizabeth GAERTNER          Sub-Investigator: Mathieu JEANNE          Sub-Investigator: Hervé MUSELLEC 收起 <<
NCT03036514 Pain, Postoperative Not Applicable Active, not recruiting February 2019 Belgium ... 展开 >> University hospital Antwerp Edegem, Antwerp, Belgium, 2650 收起 <<

Droperidol/氟哌啶 参考文献

[1]Kao LW, Kirk MA, et al. Droperidol, QT prolongation, and sudden death: what is the evidence? Ann Emerg Med. 2003 Apr;41(4):546-58.

[2]Adamantidis MM, Kerram P, et al. Droperidol exerts dual effects on repolarization and induces early afterdepolarizations and triggered activity in rabbit Purkinje fibers. J Pharmacol Exp Ther. 1993 Aug;266(2):884-93.

[3]Thomas MC, Musselman ME, Shewmaker J. Droperidol for the treatment of acute migraine headaches. Ann Pharmacother. 2015;49(2):233‐240

[4]Perkins J, Ho JD, Vilke GM, DeMers G. American Academy of Emergency Medicine Position Statement: Safety of Droperidol Use in the Emergency Department. J Emerg Med. 2015;49(1):91‐97

[5]Taylor DM, Yap CYL, Knott JC, et al. Midazolam-Droperidol, Droperidol, or Olanzapine for Acute Agitation: A Randomized Clinical Trial. Ann Emerg Med. 2017;69(3):318‐326.e1

[6]McKeage K, Simpson D, Wagstaff AJ. Intravenous droperidol: a review of its use in the management of postoperative nausea and vomiting. Drugs. 2006;66(16):2123‐2147

Droperidol/氟哌啶 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.64mL

0.53mL

0.26mL

13.18mL

2.64mL

1.32mL

26.36mL

5.27mL

2.64mL

Droperidol/氟哌啶 技术信息

CAS号548-73-2
分子式C22H22FN3O2
分子量 379.43
SMILES Code O=C1NC2=CC=CC=C2N1C3=CCN(CCCC(C4=CC=C(F)C=C4)=O)CC3
MDL No. MFCD00083290
别名 氟哌利多 ;Dehydrobenzperidol; DHBP; Taylor Brand of Droperidol; Kern Brand of Droperidol; Janssen Brand of Droperidol; Properidol; Dridol; Inapsine; Droleptan; NSC 169874
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C
溶解方案

DMSO: 35 mg/mL(92.24 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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二

Tags: Droperidol | 548-73-2 | Dehydrobenzperidol | Dopamine Receptor | Dopamine Receptor Antagonist | GPCR/G Protein | Neuronal Signaling | Dopamine Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Droperidol/氟哌啶 纯度/质量文件 | Droperidol/氟哌啶 亚型比较 | Droperidol/氟哌啶 生物活性 | Droperidol/氟哌啶 临床数据 | Droperidol/氟哌啶 参考文献 | Droperidol/氟哌啶 实验方案 | Droperidol/氟哌啶 技术信息

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