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胃复安 /Metoclopramide {[allProObj[0].p_purity_real_show]}

货号:A127869 同义名: 甲氧氯普胺

Metoclopramide is an antagonist of dopamine D2 and is commonly used as an antiemetic.

Metoclopramide 化学结构 CAS号:364-62-5
Metoclopramide 化学结构
CAS号:364-62-5
Metoclopramide 3D分子结构
CAS号:364-62-5
Metoclopramide 化学结构 CAS号:364-62-5
Metoclopramide 3D分子结构 CAS号:364-62-5
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Metoclopramide 纯度/质量文件 产品仅供科研

货号:A127869 标准纯度: {[allProObj[0].p_purity_real_show]}
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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 ++

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

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。

Metoclopramide 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].

Metoclopramide 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 <<

Metoclopramide 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

Metoclopramide 实验方案

计算器
存储液制备 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

Metoclopramide 技术信息

CAS号364-62-5
分子式C14H22ClN3O2
分子量 299.796
别名 甲氧氯普胺
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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
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