S80109 |
Mosapride |
源葉(MedMol) | 98% |
- 產(chǎn)品描述: Mosapride是胃動力藥,是選擇性的5HT4激動劑
- 靶點(diǎn): 5HT4;5-HTReceptor
- 體外研究:
Mosapride facilitates acetylcholine release from the enteric cholinergic neurons. It does not block K+ channels or D2 dopaminergic receptors. Mosapride is a selective 5-HT4 receptor agonist with no affinity for 5-HT1, 5-HT2, adrenalineα1, adrenalineα2 or dopamine D2 receptors
- 體內(nèi)研究:
Mosapride augmented lower gastrointestinal motility in animal models and in patients with lower gastrointestinal disorders. It enhanced defecation responses in animal models. In human, after oral administration of single doses of mosapride 5-40 mg, peak mosapride concentrations (Cmax) were reached after about 1 hour. Both the Cmax and area under the concentration-time curve from time zero to infinity (AUC∞) increased in a dose-proportional manner. There were no significant differences in the pharmacokinetic profiles of mosapride administered as single or multiple doses. Mosapride is excreted in the urine and faeces. It is primarily metabolized in the liver by cytochrome P450 3A4 to the active metabolite, a des-4-fluorobenzyl compound
- 動物實(shí)驗(yàn): Animal Models: Male Hartley guinea pigs Dosages: 3, 10 and 30 mg/kg Administration: i.g.
- 參考文獻(xiàn):
1. Inui A, et al. Effects of mosapride citrate, a 5-HT4 receptor agonist, on colonic motility in conscious guinea pigs. Jpn J Pharmacol. 2002, 90(4):313-20. 2. Liu Z, et al. Mosapride citrate, a novel 5-HT4 agonist and partial 5-HT3 antagonist, ameliorates constipation in parkinsonian patients. Mov Disord. 2005, 20(6):680-6. 3. Monique P. Curran, et al. Mosapride. Drugs (2008) 68: 981.
- 溶解性: soluble in DMSO
- 保存條件: -20℃
- 備注: Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist. Target: 5HT4 Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist. The major active metabolite of mosapride, known as M1, additionally acts as a 5HT3 antagonist, which accelerates gastric emptying throughout the whole of the gastrointestinal tract in humans, and is used for the treatment of gastritis, gastro-oesophageal reflux disease, functional dyspepsia and irritable bowel syndrome. It is recommended to be
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 2.37 ml 11.851 ml 23.703 ml 5 mM 0.474 ml 2.37 ml 4.741 ml 10 mM 0.237 ml 1.185 ml 2.37 ml 50 mM 0.047 ml 0.237 ml 0.474 ml
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輸入產(chǎn)品批號:
本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)