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Alizapride HCl

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Chemical Structure| 59338-87-3 同义名 : Alizapride (hydrochloride);Alizapride hydrochloride
CAS号 : 59338-87-3
货号 : A201469
分子式 : C16H22ClN5O2
纯度 : 99+%
分子量 : 351.831
MDL号 : MFCD02183928
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
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：
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].
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 - -
实验方案
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
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