产品说明书

Metoclopramide

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Chemical Structure| 364-62-5 同义名 : 甲氧氯普胺
CAS号 : 364-62-5
货号 : A127869
分子式 : C14H22ClN3O2
纯度 : 99+%
分子量 : 299.796
MDL号 : MFCD00211338
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(350.24 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
动物实验配方：
生物活性
靶点

  • Dopamine receptor

  • D2 receptor
描述 Metoclopramide acts on several different receptors; primarily as a dopamine receptor antagonist, both peripherally improving gastric emptying, and centrally resulting in an anti-emetic effect. Metoclopramide side effects, mostly related to its ability to cross the blood-brain barrier, include drowsiness, restlessness, hyperprolactinemia, and tardive dyskinesia (TD), a movement disorder that may be irreversible[3]. Intranasal metoclopramide 80 mg significantly reduced the frequency of acute vomiting in 43 patients receiving highly emetogenic chemotherapy. Intranasal metoclopramide caused minor irritation of the nasal membrane and unpleasant taste in some patients, but was otherwise well tolerated[4]. Metoclopramide's effect on the medullary chemoreceptor trigger zone makes it useful as a routine anti-emetic and in preventing vomiting induced by antineoplastic drugs, particularly cisplatin. Metoclopramide's gastrointestinal smooth muscle stimulatory effects are related to its ability to antagonize the inhibitory neurotransmitter, dopamine; to augment acetylcholine release and sensitize the muscarinic receptors of the gastrointestinal smooth muscle; and to coordinate gastric-pyloric-small intestinal motor function[5]. Patients with severe migraine attacks treated with metoclopramide as monotherapy showed a significant improvement in terms of pain relief and a faster improvement in pain intensity compared to those treated with paracetamol[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
NCT02627950 Acute Myocardial Infarction Phase 4 Unknown September 2017 Germany ... 展开 >> University of Luebeck Recruiting Luebeck, Germany, 23538 Contact: Holger Thiele       holger.thiele@uksh.de    Contact: Roza Meyer-Saraei       roza.meyer-saraei@uksh.de    Principal Investigator: Holger Thiele 收起 <<
NCT00817934 - Unknown January 2010 United States, Delaware ... 展开 >> Cedar Tree Surgical Center Millsboro, Delaware, United States, 19966 收起 <<
NCT00977223 Healthy Volunteers Phase 4 Completed - France ... 展开 >> Rouen Clinical research Centre (CIC 0204) Rouen, Haute Normandie, France, 76031 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.34mL

0.67mL

0.33mL

16.68mL

3.34mL

1.67mL

33.36mL

6.67mL

3.34mL
参考文献

[1]Navari RM, Nagy CK, Gray SE. The use of olanzapine versus metoclopramide for the treatment of breakthrough chemotherapy-induced nausea and vomiting in patients receiving highly emetogenic chemotherapy. Support Care Cancer. 2013 Jan 12.

[2]Matok I, Gorodischer R, et al. The safety of metoclopramide use in the first trimester of pregnancy. N Engl J Med. 2009 Jun 11;360(24):2528-35.

[3]Shakhatreh M, Jehangir A, Malik Z, Parkman HP. Metoclopramide for the treatment of diabetic gastroparesis. Expert Rev Gastroenterol Hepatol. 2019;13(8):711‐721

[4]Ormrod D, Goa KL. Intranasal metoclopramide. Drugs. 1999;58(2):315‐324

[5]Albibi R, McCallum RW. Metoclopramide: pharmacology and clinical application. Ann Intern Med. 1983;98(1):86‐95

[6]Salazar G, Fragoso M, Vergez L, Sergio P, Cuello D. Metoclopramide as an analgesic in severe migraine attacks: an open, single-blind, parallel control study. Recent Pat CNS Drug Discov. 2011;6(2):141‐145