新型止泻药盐酸利达脒（WHR-1142A）的作用机制研究
Mechanism of action studies of lidamidine hydrochloride (WHR-1142A), a novel antidiarrheal agent.
作者信息
Mir G N, Sperow J W, Krebs J B, Eash J R, Rowles G S, Yelnosky J
出版信息
Arzneimittelforschung. 1978;28(8a):1454-61.
1-(2,6-Dimethylphenyl)-3-methylamidinourea hydrochloride (WHR-1142A), lidamidine hydrochloride), a novel antidiarrheal agent, inhibited contractile activity in isolated guinea pig ileum stimulated by acetylcholine, histamine, serotonin, dimethylphenylpiperazinium, prostaglandin E2, BaCl2 and KCl. WHR-1142A also blocked spontaneous and stimulated contractile activity measured with extraluminal strain gauges in the duodenum, ileum and colon of dogs. Studies on the autonomic effects of WHR-1142A indicated little, if any, peripheral adrenergic stimulatory or cholinergic blocking activity. Inhibition of intestinal motility by WHR-1142A was not antagonized by naloxone. WHR-1142A also showed no morphine-like analgesic effects and was devoid of any H1-antihistamine activity. WHR-1142A appears to be a pharmacologically unique antidiarrheal agent.
1-（2,6-二甲基苯基）-3-甲基脒基脲盐酸盐（WHR-1142A，盐酸利达脒），一种新型止泻药，可抑制由乙酰胆碱、组胺、5-羟色胺、二甲基苯基哌嗪鎓、前列腺素E2、氯化钡和氯化钾刺激的豚鼠离体回肠的收缩活性。WHR-1142A还可阻断用外置应变仪在犬十二指肠、回肠和结肠中测量的自发性和刺激性收缩活性。对WHR-1142A自主神经效应的研究表明，其几乎没有外周肾上腺素能刺激或胆碱能阻断活性（若有也微乎其微）。纳洛酮不能拮抗WHR-1142A对肠道运动的抑制作用。WHR-1142A也未表现出类吗啡镇痛作用，且无任何H1-抗组胺活性。WHR-1142A似乎是一种药理学特性独特的止泻药。
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