Metoclopramide is an antagonist of dopamine D2 and is commonly used as an antiemetic.
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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。 |
靶点 |
|
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]. |
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 << |
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 |
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 |