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盐酸阿立必利 /Alizapride HCl {[allProObj[0].p_purity_real_show]}

货号：A201469 同义名： Alizapride (hydrochloride);Alizapride hydrochloride

Alizapride HCl is a dopamine receptor antagonist used in the administration of nausea and vomiting.

Alizapride HCl 化学结构 CAS号：59338-87-3
Alizapride HCl 化学结构
CAS号：59338-87-3
Alizapride HCl 3D分子结构
CAS号：59338-87-3
Alizapride HCl 化学结构 CAS号：59338-87-3
Alizapride HCl 3D分子结构 CAS号：59338-87-3
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Alizapride HCl 纯度/质量文件 产品仅供科研

货号：A201469 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

 		98%
Tetrahydroberberine,THB +

D2 receptor, pKi: 6.08

 		98+%
Prochlorperazine Maleate ✔ 95%
Olanzapine ✔ 99+%
Trifluoperazine ++++

Dopamine D2 receptor, IC50: 1.1 nM

 		98%
Ropinirole hydrochloride ++

D2 receptor, Ki: 29 nM

 		99%
Lurasidone ++++

D2 receptor, Ki: 1 nM

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

D2 receptor, Ki: 1.4 nM

 		99%
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

 		98+%
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 ✔ 97%
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

 		99%
Chlorprothixene +++

D1 receptor, Ki: 18 nM

 		+++

D2 receptor, Ki: 2.96 nM

 		+++

D3 receptor, Ki: 4.56 nM

 		+++

D5 receptor, Ki: 9 nM

 		98%
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。

Alizapride HCl 生物活性

靶点

  • Dopamine receptor
描述 Alizapride (Hydrochloride) is a potent antiemetic, acting as a dopamine receptor antagonist on the chemoreceptor trigger zone with few gastrokinetic properties. Alizapride can be proposed as an antiemetic in patients with biliary disorders[3]. Alizapride (Hydrochloride) is a methoxy-2-benzamide derivative three times more potent than its parent compound, metoclopramide, as an antagonist of apomorphine-induced emesis in dogs. Alizapride is more active than placebo when combined with DXM (dexamethasone) for DDP-induced (cisplatin) emesis in patients at high risk of severe nausea and vomiting[4]. In early clinical trials alizapride showed a better antiemetic activity with fewer side effects than metoclopramide. Alizapride has antiemetic activity and few side effects in the dose of 4 mg/kg x 5[5]. The incidence of nausea and vomiting was lower with the alizapride-treated patients, while, contrary to the experience with other antiemetics, prolonged recovery was not observed. Alizapride 100 to 200 mg intravenously is efficacious in the prevention of postoperative nausea and vomiting[6].

Alizapride HCl 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
NCT02704182 Knee Replacement Not Applicable Completed - -
NCT03178708 Spinal Curvatures Phase 2 Phase 3 Recruiting October 30, 2018 Egypt ... 展开 >> Assiut governorate Recruiting Assiut, Egypt Contact: Ghada M Aboelfadl, MD    01005802086    ghadafadl77@gmail.com 收起 <<
NCT01636947 - Completed - -

Alizapride HCl 参考文献

[1]Aprile S, Del Grosso E, et al. In vitro metabolic fate of alizapride: evidence for the formation of reactive metabolites based on liquid chromatography-tandem mass spectrometry. J Mass Spectrom. 2012 Jun;47(6):737-50.

[2]Dhasmana KM, Villalon CM, et al. The role of dopamine (D2), alpha and beta-adrenoceptor receptors in the decrease in gastrointestinal transit induced by dopamine and dopamine-related drugs in the rat. Pharmacol Res. 1993 May-Jun;27(4):335-47.

[3]Warzee PL, Dive CC. Manometric study of the activity of alizapride on the motor function of the human sphincter of Oddi. J Clin Pharm Ther. 1988;13(4):281‐284

[4]Bleiberg H, Gerard B, Dalesio O, Crespeigne N, Rozencweig M. Activity of a new antiemetic agent: alizapride. A randomized double-blind crossover controlled trial. Cancer Chemother Pharmacol. 1988;22(4):316‐320

[5]Joss RA, Galeazzi RL, Bischoff AK, Brunner KW. Alizapride, a new substituted benzamide, as an antiemetic during cancer chemotherapy. Eur J Clin Pharmacol. 1985;27(6):721‐725

[6]Booij LH, Rachmat S, Bulder ER. Alizapride in prevention of postoperative nausea and vomiting. Neth J Surg. 1988;40(1):6‐9

Alizapride HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.84mL

0.57mL

0.28mL

14.21mL

2.84mL

1.42mL

28.42mL

5.68mL

2.84mL

Alizapride HCl 技术信息

CAS号59338-87-3
分子式C16H22ClN5O2
分子量 351.831
别名 Alizapride (hydrochloride);Alizapride hydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C
溶解度

DMSO: 35 mg/mL(99.48 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: 100 mg/mL(284.23 mM)，配合低频超声助溶
动物实验配方

Tags: Alizapride | 59338-87-3 | D2 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 | Alizapride HCl 纯度/质量文件 | Alizapride HCl 亚型比较 | Alizapride HCl 生物活性 | Alizapride HCl 临床数据 | Alizapride HCl 参考文献 | Alizapride HCl 实验方案 | Alizapride HCl 技术信息

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