Johnson L R, Guthrie P D
Am J Physiol. 1984 Jan;246(1 Pt 1):G62-6. doi: 10.1152/ajpgi.1984.246.1.G62.
Proglumide, a glutaramic acid derivative, inhibits the acid secretory effects of gastrin and is said to be a specific gastrin receptor blocking agent. In the current study we have shown that proglumide inhibits the binding of gastrin to its receptor in rat oxyntic gland mucosa and tested whether this receptor is also responsible for the trophic effect of gastrin. In the first study 400 mg/kg proglumide injected with 250 micrograms/kg pentagastrin every 8 h for 48 h totally prevented the trophic effects of pentagastrin in rat oxyntic gland mucosa. Parameters measured included DNA synthesis and DNA, RNA, and protein content. In a second study the lowest maximally effective dose of proglumide was determined to be 100 mg/kg. The trophic effect of pentagastrin was inhibited in duodenal mucosa, colonic mucosa, and pancreas as well as oxyntic gland mucosa. These data demonstrate that proglumide blocks the trophic action of exogenous gastrin and suggest that the trophic effect of gastrin is mediated by the gastrin receptor.
丙谷胺是一种谷氨酸衍生物，可抑制胃泌素的泌酸作用，据说是一种特异性胃泌素受体阻断剂。在本研究中，我们发现丙谷胺可抑制胃泌素与其在大鼠胃底腺黏膜中受体的结合，并测试了该受体是否也介导胃泌素的营养作用。在第一项研究中，每8小时注射400mg/kg丙谷胺与250μg/kg五肽胃泌素，持续48小时，完全阻断了五肽胃泌素对大鼠胃底腺黏膜的营养作用。所测量的参数包括DNA合成以及DNA、RNA和蛋白质含量。在第二项研究中，确定丙谷胺的最低最大有效剂量为100mg/kg。五肽胃泌素对十二指肠黏膜、结肠黏膜、胰腺以及胃底腺黏膜的营养作用均受到抑制。这些数据表明，丙谷胺可阻断外源性胃泌素的营养作用，并提示胃泌素的营养作用是由胃泌素受体介导的。
