Gerner T, Haffner J F
Scand J Gastroenterol. 1978;13(7):789-94. doi: 10.3109/00365527809182192.
Pressure responses to cholecystokinin (CCK-PZ, approximately 500 U/mg) and gastrin (human synthetic gastrin) were investigated in isolated guinea-pig antral and fundal pouches. Both drugs stimulated motor activity, in the antrum mainly by increasing amplitudes and rhythmic activity, in the fundus by increasing basal tension. Antral responses to gastrin were markedly smaller than to CCK-PZ, while the differences were less pronounced in the fundus. Prestimulation with gastrin, being an agonist by itself, significantly reduced the antral responses to submaximal doses of CCK-PZ, while no inhibition was found in the fundus. When pre-exposed to gastrin, the antral dose-response curve to CCK-PZ was flattened, with reduced maximal response, simulating a non-competitive interaction. It seems that gastrin behaves like a partial agonist to CCK-PZ on guinea-pig antral smooth muscle.
在离体豚鼠胃窦和胃底囊中研究了对胆囊收缩素(CCK - PZ,约500 U/mg)和胃泌素(人合成胃泌素)的压力反应。两种药物均刺激运动活性,在胃窦主要通过增加幅度和节律性活动,在胃底则通过增加基础张力。胃窦对胃泌素的反应明显小于对CCK - PZ的反应,而在胃底差异则不那么明显。胃泌素本身作为一种激动剂,预刺激显著降低了胃窦对次最大剂量CCK - PZ的反应,而在胃底未发现抑制作用。当预先暴露于胃泌素时,胃窦对CCK - PZ的剂量反应曲线变平,最大反应降低,模拟了一种非竞争性相互作用。胃泌素在豚鼠胃窦平滑肌上似乎表现得像CCK - PZ的部分激动剂。