Acotiamide
(Synonyms: Z-338 free base; YM443 free base) 目录号 : GC20093
Acotiamide is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with an IC50 of 1.79 μM. Acotiamide can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory
Cas No.:185106-16-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Acotiamide is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with an IC50 of 1.79 μM. Acotiamide can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory
| Cas No. | 185106-16-5 | SDF | |
| 别名 | Z-338 free base; YM443 free base | ||
| 分子式 | C21H30N4O5S | 分子量 | 450.55 |
| 溶解度 | 储存条件 | Store at 2-8°C | |
| 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 | 2.2195 mL | 11.0975 mL | 22.1951 mL |
| 5 mM | 0.4439 mL | 2.2195 mL | 4.439 mL |
| 10 mM | 0.222 mL | 1.1098 mL | 2.2195 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Acotiamide and Functional Dyspepsia: A Systematic Review and Meta-Analysis
Cureus 2021 Dec 20;13(12):e20532.PMID:35070565DOI:10.7759/cureus.20532.
Functional dyspepsia is a common gastrointestinal disorder characterized by postprandial fullness or early satiety and epigastric burning or pain in the absence of organic disease. Acotiamide is a novel prokinetic motility drug being used in functional dyspepsia. Databases like PubMed, PubMed Central, Embase, and Scopus were searched for studies comparing the use of Acotiamide and placebo for people with functional dyspepsia. Quantitative synthesis was performed using RevMan 5.4 (Cochrane, London, United Kingdom). The improvement in symptoms of functional dyspepsia after treatment was higher in people treated with Acotiamide than placebo, although not statistically significant (OR, 1.48; 95% CI, 0.93 to 2.35; n = 1697; I2 = 59%). Among the commonly reported adverse effects, namely, raised in serum prolactin (OR 1.02, 95% CI 0.64 to 1.61; n = 1709; I2 = 44%), raised in alanine transaminase (OR 1.27, 95% CI 0.70 to 2.33; n = 1709; I2 = 0%), and raised in serum bilirubin (OR, 0.98; 95% CI, 0.52 to 1.87; I2 = 0%) did not differ between two groups. Acotiamide seems to be a promising agent in functional dyspepsia. However, further larger studies are needed to evaluate the role of Acotiamide in functional dyspepsia.
Acotiamide (Z-338) as a possible candidate for the treatment of functional dyspepsia
Neurogastroenterol Motil 2010 Jun;22(6):595-9.PMID:20553562DOI:10.1111/j.1365-2982.2010.01486.x.
Acotiamide hydrochloride is a novel upper gastrointestinal (GI) motility modulator and stress regulator currently being developed for the treatment of functional dyspepsia (FD). The mechanism underlying the enhancement of GI motility by this agent has been proposed to be based on its muscarinic antagonism and inhibitory effects on acetylcholinesterase activity. Pathophysiological studies showed that Acotiamide significantly improved both delayed gastric emptying and feeding inhibition in restraint stress-induced model, but did not affect both normal gastric emptying and feeding in intact animals, indicating that Acotiamide exerted effects only on the impaired gastric emptying and feeding behavior. According to the clinical pilot study in Europe, Acotiamide, at the dose of 100 mg t.i.d., showed to improve the symptoms and quality of life of patients with FD, indicating the need for larger scale symptomatic studies on the efficacy of Acotiamide in patients with FD. The recent phase II studies conducted in Japan presented in this issue of the journal also confirmed that Acotiamide, at the optimal dose of 100 mg, has potential therapeutic efficacy, especially for meal-related FD symptoms. Although a phase III study is on going, Acotiamide is now expected as a novel treatment option for FD.
Profile of Acotiamide in the treatment of functional dyspepsia
Clin Exp Gastroenterol 2016 Apr 6;9:83-8.PMID:27103837DOI:10.2147/CEG.S72172.
Efficacy of Acotiamide for improving symptoms in patients with functional dyspepsia was shown by several clinical trials. In a randomized, double-blind, placebo-controlled, parallel-group comparative Phase III trial conducted in Japan, 100 mg of Acotiamide three times a day for 4 weeks was more effective than a placebo for improving symptoms, and quality of life. Acotiamide was well-tolerated treatment, with no significant adverse events. The aim of this review was to summarize the current evidence of the efficacy of Acotiamide in the treatment of patients with functional dyspepsia.
Acotiamide (Z-338, YM443), a new drug for the treatment of functional dyspepsia
Expert Opin Investig Drugs 2011 May;20(5):701-12.PMID:21417958DOI:10.1517/13543784.2011.562890.
Introduction: Functional dyspepsia (FD) is a highly prevalent condition with a major impact on quality of life and high socio-economic and healthcare costs. To date, no treatment of established efficacy in FD is available. Acotiamide (Z-338 or YM443) is a new drug under development for the treatment of FD. Areas covered: Acotiamide is a gastroprokinetic drug that enhances acetylcholine release in the enteric nervous system via muscarinic receptor antagonism and acetycholinesterase inhibition. In conscious rats and dogs, Acotiamide enhanced gastric contractility and accelerated delayed gastric emptying. Although in healthy volunteers Acotiamide did not affect gastric emptying, gastric emptying and gastric accommodation were enhanced in FD. Acotiamide was evaluated in FD in several clinical studies in different countries and these are supportive of a symptomatic benefit. The beneficial effect is most consistently found with the 100 mg dose (three times a day) and primarily involves the postprandial distress syndrome symptoms of postprandial fullness, early satiety and upper abdominal bloating. The mechanism underlying the symptomatic benefit with Acotiamide is not fully established but may involve enhanced gastric accommodation and increased gastric emptying. Expert opinion: Compared to placebo, no adverse events have been reported in the current short-term studies, while Acotiamide seems efficacious for treating postprandial distress syndrome symptoms in FD patients.
Acotiamide, a novel gastroprokinetic for the treatment of patients with functional dyspepsia: postprandial distress syndrome
Expert Rev Gastroenterol Hepatol 2012 Sep;6(5):533-44.PMID:23061703DOI:10.1586/egh.12.34.
Functional dyspepsia (FD) is a highly prevalent condition with major socioeconomic and healthcare impact. To date, no pharmacological treatment for FD has been approved. The Rome consensus proposed to subdivide FD into postprandial distress syndrome (PDS), characterized by meal-related symptoms and epigastric pain syndrome, characterized by pain and burning. Acotiamide (Z-338 or YM443) is a new drug, developed for the treatment of FD. Acotiamide enhances acetylcholine release from enteric neurons through muscarinic receptor antagonism and acetycholinesterase inhibition, thereby enhancing gastric emptying and gastric accommodation. Acotiamide was evaluated in FD in clinical studies in Europe, Japan and the USA, beneficial effects were observed for the PDS symptoms of postprandial fullness and early satiation, with a dose of 100 mg three-times a day. A 4-week placebo-controlled Phase III study in PDS patients in Japan confirmed efficacy of Acotiamide in relieving postprandial fullness, early satiation and upper abdominal bloating.