| Description | Lidamidine (Lidamidinum) is an effective antidiarrheal agent that inhibits intestinal secretion, reduces intestinal transit, and inhibits smooth muscle contraction. |
| In vivo | 禁食的雄性大鼠在麻醉状态下，安装了一根位于上升结肠开始的10cm液体充满段的内腔插管（基础压力为10 cm H2O）。内腔压力通过连接到封闭液体系统的换能器监测。所有化合物都通过缓慢静脉输注给药。在70分钟的时间里，观察到一种规律的明显收缩复合体模式。这些收缩使内腔压力增加到39 +/- 1.2 cm H2O（平均值 +/- 标准误），频率为每分钟0.3次，持续时间从1分钟到2.5分钟。使用阿托品（0.1 mg/kg）或Lidamidine （3.0 mg/kg）观察到这些收缩模式的抑制。伊达唑安（3.0 mg/kg）的20分钟预处理对Lidamidine 的效果产生了拮抗作用，但对阿托品的作用无影响。Trimazosin（1 mg/kg）或普萘洛尔（0.3 mg/kg）的预处理未能拮抗Lidamidine 产生的抑制[1]。 |
| Synonyms | Lidamidina, Lidamidinum, 利达脒 |
| molecular weight | 220.27 |
| Molecular formula | C11H16N4O |
| CAS | 66871-56-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 5 mg/mL (22.7 mM) |
| References | 1. Eaker EY, Bixler GB, Mathias JR. WHR 1049, a potent metabolite of lidamidine, has antidiarrheal and antimotility effects on the small intestine in rats. J Pharmacol Exp Ther. 1988 Aug;246(2):786-9. PubMed PMID: 3404458. 2. Wienbeck M, Bohn M. Different actions of 2 antidiarrheal agents, lidamidine and loperamide, on motility of the isolated cat colon muscle. Z Gastroenterol. 1985 Apr;23(4):175-82. PubMed PMID: 4060808. 3. Awad RA, Llorens F, Camelo AL, Sánchez M. A randomised double-blind placebo-controlled trial of lidamidine HCL in irritable bowel syndrome. Acta Gastroenterol Latinoam. 2000;30(3):169-75. PubMed PMID: 10975022. 4. Bleakman D, Naftalin RJ. Prevention of guanine nucleotide-induced reductions in muscarinic agonist binding to rabbit ileal submucosal membranes by lidamidine and tetracaine. Naunyn Schmiedebergs Arch Pharmacol. 1988 Apr;337(4):366-72. PubMed PMID: 2900471. |