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/ 多巴胺受体 / Metoclopramide/胃复安

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

货号：A127869 同义名： 甲氧氯普胺

Metoclopramide 是一种 5-HT3 和多巴胺 D2 受体拮抗剂（IC50 值分别为 308 nM 和 483 nM），用于恶心、呕吐及胃食管反流的研究。

Metoclopramide/胃复安 化学结构 CAS号：364-62-5
Metoclopramide/胃复安 化学结构
CAS号：364-62-5
Metoclopramide/胃复安 3D分子结构
CAS号：364-62-5
Metoclopramide/胃复安 化学结构 CAS号：364-62-5
Metoclopramide/胃复安 3D分子结构 CAS号：364-62-5
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Metoclopramide/胃复安 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]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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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。

Metoclopramide/胃复安 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/胃复安 细胞实验

Cell Line
Concentration Treated Time Description References
FO B cells 50 ng/mL 48 h PRL promoted the differentiation of FO B cells into B-GCs Front Immunol. 2022 Oct 25;13:1017115.
B cells 50 ng/mL 48 h PRL increased the percentage of B-GCs in MRL/lpr mice Front Immunol. 2022 Oct 25;13:1017115.
BHK-21 cells 200 µM 24 h To evaluate the antiviral efficacy of Metoclopramide against DENV infection. Results showed that Metoclopramide did not significantly affect BHK-21 cells, likely due to lower D2R expression in BHK-21 cells. Front Cell Infect Microbiol. 2021 Feb 2;10:606743.
Neuro-2a cells 200 µM 24 h To evaluate the antiviral efficacy of Metoclopramide against DENV infection. Results showed that Metoclopramide significantly reduced viral titers in Neuro-2a cells. Front Cell Infect Microbiol. 2021 Feb 2;10:606743.
MDCKII-MDR1 cells 4 nM 30 min To test the inhibitory effect of Tariquidar on P-gp, results showed that [11C]metoclopramide was the most sensitive to P-gp inhibition 2022 Jan;42(1):175-185. doi: 10.1177/0271678X211045444.

Metoclopramide/胃复安 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice KC mice Subcutaneous injection 100 μg Once daily for 3 weeks To study the effect of Metoclopramide on PanIN progression, results showed that Metoclopramide-treated mice had increased serum prolactin levels, which promoted PanIN progression. Cancer Res. 2019 Oct 15;79(20):5316-5327
Mice MRL/lpr mice Subcutaneous injection 200 µg Five doses per week for six weeks Metoclopramide increased PRL levels in MRL/lpr mice and elevated anti-dsDNA IgG3 autoantibody levels Front Immunol. 2022 Oct 25;13:1017115.
Swiss albino mice Gastric emptying and gastrointestinal transit experiment Oral 30 mg/kg Single administration To evaluate the interaction of AoEF with metoclopramide, serotonin, and carbachol on gastric emptying and gastrointestinal transit. Results showed that pretreatment with AoEF significantly inhibited the action of carbachol on gastric emptying and gastrointestinal transit, but had no significant effect on the action of serotonin and metoclopramide. J Pharm Anal. 2021 Dec;11(6):776-782
ICR suckling mice DENV infection model Intracerebral and intraperitoneal injections 1 mg/kg Single dose, duration of 9 days To evaluate the antiviral efficacy of Metoclopramide against DENV-induced CNS neuropathy and mortality. Results showed that Metoclopramide significantly reduced DENV-induced disease progression and mortality. Front Cell Infect Microbiol. 2021 Feb 2;10:606743.
Sprague Dawley rats DNBS-induced colitis model Oral gavage 6.7 mg/kg and 33.8 mg/kg Once daily for 7 days To evaluate the efficacy of MCP-azo-ASA on DNBS-induced colitis, results showed that MCP-azo-ASA significantly alleviated colonic damage and inflammation Drug Des Devel Ther. 2018 Dec 28;13:231-242
ICR mice Metoclopramide-induced hyperprolactinemia model Intraperitoneal injection 20 mg/kg Once every 2 days for 21 days To assess the effect of HY7801 on metoclopramide-induced hyperprolactinemia in mice, results showed that HY7801 significantly reduced prolactin levels, regulated sex hormone and prostaglandin levels, and suppressed the expression of inflammatory markers. Nutrients. 2024 Nov 14;16(22):3889.
Rats Sprague Dawley rats Intravenous injection 1 mg/kg Single injection, lasting 30 minutes To evaluate the inhibitory effect of Tariquidar on P-gp, results showed that 1 mg/kg Tariquidar increased the brain exposure of [11C]metoclopramide by 2.1-fold 2022 Jan;42(1):175-185. doi: 10.1177/0271678X211045444.

Metoclopramide/胃复安 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/胃复安 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/胃复安 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/胃复安 技术信息

CAS号364-62-5
分子式C14H22ClN3O2
分子量 299.8
SMILES Code O=C(NCCN(CC)CC)C1=CC(Cl)=C(N)C=C1OC
MDL No. MFCD00211338
别名 甲氧氯普胺
运输蓝冰
InChI Key TTWJBBZEZQICBI-UHFFFAOYSA-N
Pubchem ID 4168
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C
溶解方案

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

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: Metoclopramide | 甲氧氯普胺 | Dopamine Receptor | AmBeed-信号通路专用抑制剂 | Metoclopramide/胃复安 纯度/质量文件 | Metoclopramide/胃复安 亚型比较 | Metoclopramide/胃复安 生物活性 | Metoclopramide/胃复安 临床数据 | Metoclopramide/胃复安 参考文献 | Metoclopramide/胃复安 实验方案 | Metoclopramide/胃复安 技术信息

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