Mir G N, Alioto R L, Sperow J W, Eash J R, Krebs J B, Yelnosky J
Arzneimittelforschung. 1978;28(8a):1448-54.
1-(2,6-Dimethylphenyl)-3-methyl-amidinourea hydrochloride (WHR-1142A, lidamidine hydrochloride) was shown to have potent antimotility, antidiarrheal and intestinal antisecretory activity in mice, rats and dogs. Antimotility activity was demonstrated in charcoal intestinal motility, gastric emptying and gastric and intestinal intraluminal pressure studies. Antidiarrheal activity was evaluated in castor oil-, prostaglandin E2-, carbachol-, and serotonin-induced diarrhea. Intestinal secretion induced by cholera toxin was inhibited by WHR-1142A. In general, WHR-1142A was more potent than diphenoxylate and loperamide although species differences were noted. The ED50 for inhibition of castor oil-induced diarrhea was 1.8 mg/kg p.o. and the duration of action at 16 mg/kg p.o. was at least 6 h. Unlike diphenoxylate, WHR-1142A showed no tolerance.
1-(2,6-二甲基苯基)-3-甲基脒基脲盐酸盐（WHR-1142A，盐酸利达脒）在小鼠、大鼠和犬中显示出强效的抗蠕动、止泻和肠道抗分泌活性。在木炭肠道蠕动、胃排空以及胃和肠道腔内压力研究中证实了其抗蠕动活性。在蓖麻油、前列腺素E2、卡巴胆碱和5-羟色胺诱导的腹泻模型中评估了其止泻活性。WHR-1142A可抑制霍乱毒素诱导的肠道分泌。总体而言，尽管存在种属差异，但WHR-1142A比地芬诺酯和洛哌丁胺更有效。抑制蓖麻油诱导腹泻的半数有效剂量（ED50）为口服1.8mg/kg，口服16mg/kg时的作用持续时间至少为6小时。与地芬诺酯不同，WHR-1142A未显示出耐受性。
