Vigna S R, Szecòwka J, Williams J A
Brain Res. 1985 Sep 23;343(2):394-7. doi: 10.1016/0006-8993(85)90764-4.
The abilities of the pancreatic cholecystokinin (CCK) receptor antagonists dibutyryl cyclic GMP, proglumide, benzotript, CBZ-tryptophan, CBZ-cysteine and CCK-27-32-amide to inhibit CCK binding to its receptor in the pancreas and brain of mice and guinea pigs was examined. In both species, the same relative potencies of the antagonists in brain and pancreas was seen except that dibutyryl cyclic GMP was considerably more potent on pancreas than on cerebral cortex CCK receptors. CCK-27-32-amide was the most potent inhibitor for both brain and pancreas but was more potent in the guinea pig than in the mouse. Proglumide, a relatively weak antagonist, was a more potent inhibitor of the guinea pig than of the mouse pancreas receptor. Thus, these data suggest that there are both tissue-specific and species-specific differences in CCK antagonist interactions with the CCK receptor.
研究了胰腺胆囊收缩素（CCK）受体拮抗剂二丁酰环鸟苷酸、丙谷胺、苯并曲普、CBZ-色氨酸、CBZ-半胱氨酸和CCK-27-32-酰胺抑制CCK与小鼠和豚鼠胰腺及脑中其受体结合的能力。在这两个物种中，除了二丁酰环鸟苷酸对胰腺的作用比对大脑皮层CCK受体的作用强得多外，拮抗剂在脑和胰腺中的相对效力相同。CCK-27-32-酰胺是脑和胰腺中最有效的抑制剂，但在豚鼠中比在小鼠中更有效。丙谷胺是一种相对较弱的拮抗剂，对豚鼠胰腺受体的抑制作用比对小鼠的更强。因此，这些数据表明CCK拮抗剂与CCK受体相互作用存在组织特异性和物种特异性差异。
