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Loperamide HCl

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Chemical Structure| 34552-83-5 同义名 : 盐酸洛哌丁胺 ;R-18553 hydrochloride;Loperamide (hydrochloride);R 18553;PJ 185;NSC 696356;Loperamide hydrochloride
CAS号 : 34552-83-5
货号 : A171923
分子式 : C29H34Cl2N2O2
纯度 : 99+%
分子量 : 513.499
MDL号 : MFCD00058581
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(97.37 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

H2O: 1 mg/mL(1.95 mM)，配合低频超声助溶
动物实验配方：

2% DMSO+30% PEG 300+water 2.5 mg/mL

生物活性
描述 Loperamide (Hydrochloride) is an opioid receptor agonist widely used for the treatment of diarrhea[3]. In contrast with other opioid agonists, loperamide is a peripherally acting μ-receptor agonist exerting its effects mainly on the myenteric plexus of the gastrointestinal longitudinal muscle layer. It decreases peristalsis and fluid secretion resulting in longer gastrointestinal transit time. The bioavailability of the drug is extremely low. Moreover, it is actively excluded from the central nervous system; hence, it lacks the central effects of euphoria and analgesia at the recommended dosages[4]. Rats were orally gavaged with 1.5, 3, or 6 mg/kg body weight (BW) of loperamide hydrochloride for 7 days. The results after 7 days administration of loperamide, revealed dose-dependent increase in aspartate aminotransferase, lactate dehydrogenase, creatine kinase-MB, and serum concentration of cardiac troponin I, total homocysteine, and nitric oxide. Loperamide provoked cardiotoxicity through oxidative stress, lipid peroxidation, and DNA fragmentation in rats[5]. Loperamide decreased cell viability in a dose-dependent fashion and was most effective against canine osteosarcoma cells. When co-incubated with doxorubicin, loperamide induced a synergistic cell kill in canine carcinoma cells[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03575078 Lymphoma Phase 1 Not yet recruiting August 23, 2023 -
NCT00555620 - Completed - -
NCT02677844 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.95mL

0.39mL

0.19mL

9.74mL

1.95mL

0.97mL

19.47mL

3.89mL

1.95mL
参考文献

[1]Hanauer SB. The role of loperamide in gastrointestinal disorders. Rev Gastroenterol Disord. 2008 Winter;8(1):15-20.

[2]Litovitz T, Clancy C, et al. Surveillance of loperamide ingestions: an analysis of 216 poison center reports. J Toxicol Clin Toxicol. 1997;35(1):11-9.

[3]Wu PE, Juurlink DN. Clinical Review: Loperamide Toxicity. Ann Emerg Med. 2017 Aug;70(2):245-252

[4]Akel T, Bekheit S. Loperamide cardiotoxicity: "A Brief Review". Ann Noninvasive Electrocardiol. 2018 Mar;23(2):e12505

[5]Olofinsan KA, Ajala-Lawal RA, Ajiboye TO. Loperamide-induced cardiotoxicity in rats: Evidence from cardiac and oxidative stress biomarkers. J Biochem Mol Toxicol. 2019 Apr;33(4):e22278

[6]Regan RC, Gogal RM Jr, Barber JP, Tuckfield RC, Howerth EW, Lawrence JA. Cytotoxic effects of loperamide hydrochloride on canine cancer cells. J Vet Med Sci. 2014 Dec;76(12):1563-8