Metoclopramide
(Synonyms: 胃复安) 目录号 : GC16249
Metoclopramide（胃复安）是一种有效的5-HT3和多巴胺D2受体拮抗剂，IC50 值分别为308nM和483nM。
Cas No.:364-62-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
Cell lines | L929 cells |
Preparation Method | L929 cells were treated with increasing concentrations of Metoclopramide (0.01-5.0μM , against Paraoxon) or (0.1-10μM, against Malathion) for 6h before exposure to either Paraoxon (10nM ) or Malathion (1μM ), corresponding to their IC50 values in L929 cells for an additional period of 16h and apoptosis was analyzed by flow cytometry after staining with FITC‐annexin‐V/PI. |
Reaction Conditions | 0.1-5.0μM、0.1-10μM; 6h |
Applications | Low micromolar concentrations of Metoclopramide effectively inhibited the potent apoptotic activities of Paraoxon and Malathion. |
| Animal experiment [2]: | |
Animal models | Wistar rats |
Preparation Method | Forty rats were divided into two groups of 20 rats each, receiving either Metoclopramide (experimental group: E) or saline (control group: C). Each group was further divided into subgroups of 10 rats each, which were sacrificed on the third (E3 and C3) or seventh (E7 and C7) postoperative day. Animals in group E were given subcutaneous Metoclopramide at a daily dose of 10mg/kg body weight every 12h until the day of euthanasia. Animals in group C were also given the same amount of saline every 12h in the same manner. Left colon segmental resection followed by end-to-end anastomosis was performed. Sepsis was induced by cecal ligation and puncture. On the day of reoperation, the total number of adhesions was assessed, and the anastomosed intestinal segments were resected for tensile strength testing, histopathological analysis, measurement of hydroxyproline levels, and histomorphometric evaluation of collagen. |
Dosage form | 10mg/kg, every 12h until the day of euthanasia; s.c. |
Applications | Number of intra-abdominal adhesions in the anastomosed area, and tensile strength before anastomosis rupture were similar among all subgroups. On the third postoperative day, the anastomoses of animals treated with Metoclopramide showed significantly lower hydroxyproline levels when compared with controls. Collagen content was similar among all subgroups. |
References: [1]Jaber B M, Petroianu G A, Rizvi S A, et al. Protective effect of metoclopramide against organophosphate‐induced apoptosis in the murine skin fibroblast L929[J]. Journal of Applied Toxicology, 2018, 38(3): 329-340. [2]e Silva S M, Carneiro F P, Ferreira V M M, et al. Effects of metoclopramide on healing of colonic anastomoses in a rat model of abdominal sepsis[J]. Journal of Investigative Surgery, 2013, 26(5): 235-241. | |
Metoclopramide is a potent 5-HT3 and dopamine D2 receptor antagonist with IC50 values of 308nM and 483nM, respectively[1]. Metoclopramide can be used in the study of nausea and vomiting, gastroesophageal reflux and gastroparesis[2]. Metoclopramide has the effect of stimulating serotonin receptors[3].
In vitro, Metoclopramide (0-10μM) treated mouse skin fibroblasts (L929 cells) for 6h effectively inhibited the potent apoptotic activity of paraoxon and malathion[4]. Metoclopramide (1μM) treated leukemia cell line (K562 cells) blocked CD93 signaling and reduced leukemia stem cell (LSC) function[5].
In vivo, Metoclopramide (10mg/kg) was injected subcutaneously to treat experimental abdominal sepsis in rats and had no adverse effects on the healing of intestinal anastomosis. The hydroxyproline level of the anastomosis was significantly reduced on the third day after surgery[6]. Metoclopramide (6.7mg/kg) was administered subcutaneously to unmated female Swiss ZH-1 mice for 50 days and significantly increased the number and volume of pituitary lactotrophs at all stages of the estrous cycle[7].
References:
[1] Hirokawa Y, Harada H, Yoshikawa T, et al. Synthesis and structure–activity relationships of 4-amino-5-chloro-N-(1, 4-dialkylhexahydro-1, 4-diazepin-6-yl)-2-methoxybenzamide derivatives, novel and potent serotonin 5-HT3 and dopamine D2 receptors dual antagonist[J]. Chemical and pharmaceutical bulletin, 2002, 50(7): 941-959.
[2] Lee A, Kuo B. Metoclopramide in the treatment of diabetic gastroparesis[J]. Expert review of endocrinology & metabolism, 2010, 5(5): 653-662.
[3] Guillemot J, Compagnon P, Cartier D, et al. Metoclopramide stimulates catecholamine-and granin-derived peptide secretion from pheochromocytoma cells through activation of serotonin type 4 (5-HT4) receptors[J]. Endocrine-Related Cancer, 2009, 16(1): 281.
[4] Jaber B M, Petroianu G A, Rizvi S A, et al. Protective effect of metoclopramide against organophosphate‐induced apoptosis in the murine skin fibroblast L929[J]. Journal of Applied Toxicology, 2018, 38(3): 329-340.
[5] Riether C, Radpour R, Kallen N M, et al. Metoclopramide treatment blocks CD93-signaling-mediated self-renewal of chronic myeloid leukemia stem cells[J]. Cell reports, 2021, 34(4).
[6] e Silva S M, Carneiro F P, Ferreira V M M, et al. Effects of metoclopramide on healing of colonic anastomoses in a rat model of abdominal sepsis[J]. Journal of Investigative Surgery, 2013, 26(5): 235-241.
[7] Gomes R C T, Verna C, Simoes R S, et al. Effects of metoclopramide on the mouse anterior pituitary during the estrous cycle[J]. Clinics, 2011, 66: 1101-1104.
Metoclopramide（胃复安）是一种有效的5-HT3和多巴胺D2受体拮抗剂，IC50 值分别为308nM和483nM[1]。Metoclopramide可用于恶心呕吐、胃食管反流和胃轻瘫的研究[2]。Metoclopramide具有激动血清素受体的作用[3]。
在体外，Metoclopramide（0-10μM）处理小鼠皮肤成纤维细胞（L929细胞）6h，有效抑制了对氧磷和马拉硫磷的强效凋亡活性[4]。Metoclopramide（1μM）处理白血病细胞系（K562细胞），阻断了CD93信号传导，降低了白血病干细胞（LSC）功能[5]。
在体内，Metoclopramide（10mg/kg）通过皮下注射治疗实验性腹部脓毒症大鼠，对肠吻合口的愈合没有有害影响，术后第三天吻合口羟脯氨酸水平明显降低[6]。Metoclopramide（6.7mg/kg）通过皮下注射处理未交配的Swiss ZH-1品系雌性小鼠50天，在发情周期的所有阶段显著增加垂体催乳细胞的数量和体积[7]。
| Cas No. | 364-62-5 | SDF | |
| 别名 | 胃复安 | ||
| 化学名 | 4-amino-5-chloro-N-[2-(diethylamino)ethyl]-2-methoxybenzamide | ||
| Canonical SMILES | CCN(CC)CCNC(=O)C1=CC(=C(C=C1OC)N)Cl | ||
| 分子式 | C14H22ClN3O2 | 分子量 | 299.8 |
| 溶解度 | ≥ 14.99 mg/mL in DMSO, ≥ 24.6 mg/mL in EtOH with gentle warming | 储存条件 | Store at 2-8°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3356 mL | 16.6778 mL | 33.3556 mL |
| 5 mM | 0.6671 mL | 3.3356 mL | 6.6711 mL |
| 10 mM | 0.3336 mL | 1.6678 mL | 3.3356 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
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