Metoclopramide 是一种有效的5-HT3和多巴胺D2受体拮抗剂，IC50值分别为 308 nM 和 483 nM。Metoclopramide 可用于恶心呕吐、胃食管反流和胃轻瘫的研究。
| 生物活性 | Metoclopramide is a potent antagonist of5-HT3anddopamine D2 receptor, withIC50s of 308 nM and 483 nM, respectively. Metoclopramide can be used for the research of nausea and vomiting, gastro-oesophageal reflux, and gastroparesis[1][2]. |
| IC50& Target[1] | 5-HT3Receptor 308 nM (IC50) | D2Receptor 483 nM (IC50) |
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体外研究
(In Vitro) | Metoclopramide (0.01-10 μM) stimulates aldosterone release in isolated perfused rat zona glomerulosa cells[3].
Metoclopramide results in prokinesis by four mechanisms: inhibition of presynaptic D2 receptors and stimulation of presynaptic excitatory 5-HT4 receptors, thereby allowing acetylcholine (ACh) release from intrinsic cholinergic motor neurons; inhibition of D2 postsynaptic receptors; and antagonism of the presynaptic inhibition of muscarinic receptors, leading to further augmentation of ACh release[2].
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体内研究
(In Vivo) | Metoclopramide (6.7 μg/g; s.c. daily for 50 days) significantly increases the number and the volume of lactotroph cells of the pituitary gland during all phases of the estrous cycle[4].
Metoclopramide (5-40 mg/kg; i.p.) induces catalepsy and antagonizes Apomorphine induced cage climbing behaviour in mice[5].
Metoclopramide (1.25-2.5 mg/kg; i.p.) induces stereotyped cage climbing behaviour in mice[5].
| Animal Model: | Adult, virgin female mice of the Swiss EPM-1 strain[4] | | Dosage: | 6.7 μg/g | | Administration: | S.c. daily for 50 days | | Result: | Increased the number but also stimulated the metabolic activity of lactotrophs. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 110 mg/mL(366.91 mM;Need ultrasonic) 配制储备液 | 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 |
*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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制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 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.75 mg/mL (9.17 mM); Clear solution
此方案可获得 ≥ 2.75 mg/mL (9.17 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.75 mg/mL (9.17 mM); Clear solution
此方案可获得 ≥ 2.75 mg/mL (9.17 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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