Khalid P, Sharma S D, Khan M M, Rastogi A K, Kidwai J R, Mathur K B
Acta Diabetol Lat. 1986 Jul-Sep;23(3):239-42. doi: 10.1007/BF02624710.
Two synthetic analogs of CCK-4, Glp-Met-Asp-Phe-NH2 (I) and Pro-Met-Asp-Phe-NH2 (II) reported earlier to stimulate insulin release from the isolated rat pancreatic islets in vitro at concentrations as low as 10(-10) M, have now been found to be totally ineffective as glucagon releasers at concentrations as high as 10(-6) M or higher. It is evident that the replacement of Trp in CCK-4 by Glp and Pro residues leads to peptides which exhibit insulin releasing activity without stimulating the release of glucagon.
两种CCK - 4的合成类似物,即早前报道的Glp - Met - Asp - Phe - NH2(I)和Pro - Met - Asp - Phe - NH2(II),在体外低至10(-10)M的浓度下就能刺激分离的大鼠胰岛释放胰岛素,现在发现它们在高达10(-6)M或更高的浓度下作为胰高血糖素释放剂却完全无效。显然,用Glp和Pro残基取代CCK - 4中的Trp会产生具有胰岛素释放活性而不刺激胰高血糖素释放的肽。