DiJoseph J F, Taylor J A, Mir G N
Life Sci. 1984 Sep 3;35(10):1031-42. doi: 10.1016/0024-3205(84)90067-5.
Alpha-2 receptor activation mediates the inhibition of a number of gastrointestinal functions including gastric and intestinal secretions. Alpha-2 receptors are located in the brain and presynaptically on cholinergic nerve terminals; activation of either inhibits vagus nerve activity. Intestinal secretions are inhibited by postsynaptic alpha-2 receptors located on intestinal epithelial cells. Agents which selectively activate alpha-2 receptors in the gut may therefore be beneficial in treating gastric ulcers and diarrheal states. Two such agents which activate alpha-2 receptors in the gut are WHR-1370A [1-n-butoxy-3-(2,6-dimethylphenylcarbamoyl) guanidine hydrochloride] and lidamidine. WHR-1370A is a potent gastric antisecretory and antiulcer agent which inhibits the release of acetylcholine from the vagus nerve. WHR-1370A's activity is blocked by yohimbine. Lidamidine is a clinically effective antidiarrheal agent. Lidamidine's response is partially inhibited by yohimbine in animal diarrheal models. Alpha-2 agonists represent a new class of drugs which have a promising future in the treatment of gastrointestinal disorders.
α2受体激活介导对包括胃和肠分泌在内的多种胃肠功能的抑制。α2受体位于脑内以及胆碱能神经末梢的突触前；二者的激活均抑制迷走神经活动。位于肠上皮细胞上的突触后α2受体抑制肠分泌。因此，选择性激活肠道α2受体的药物可能对治疗胃溃疡和腹泻状态有益。两种在肠道中激活α2受体的此类药物是WHR-1370A [1-正丁氧基-3-(2,6-二甲基苯基氨基甲酰基)胍盐酸盐]和利达脒。WHR-1370A是一种强效的胃抗分泌和抗溃疡药物，可抑制迷走神经释放乙酰胆碱。WHR-1370A的活性被育亨宾阻断。利达脒是一种临床有效的止泻药。在动物腹泻模型中，育亨宾可部分抑制利达脒的反应。α2激动剂代表一类新型药物，在胃肠疾病治疗方面有着广阔的前景。
