Rodriguez M, Galas M C, Lignon M F, Mendre C, Laur J, Aumelas A, Martinez J
Centre CNRS-INSERM de Pharmacologie-Endocrinologie, Montpellier, France.
J Med Chem. 1989 Oct;32(10):2331-9. doi: 10.1021/jm00130a018.
Syntheses of some partially modified retro-inverso analogues of the C-terminal octa- or heptapeptide of cholecystokinin are described. These analogues (in which the C-terminal carboxamide was deleted or not) were obtained by reverting one or several peptide bonds in the parent molecule. All these compounds were able to inhibit binding of labeled CCK-8 to rat pancreatic acini and guinea pig brain membranes and to stimulate amylase release from rat pancreatic acini with various potencies. Some of these derivatives reproduce only part of the biological response of CCK on amylase release.
描述了一些胆囊收缩素C端八肽或七肽的部分修饰反向类似物的合成。这些类似物（其中C端羧酰胺被删除或未被删除）是通过使母体分子中的一个或几个肽键反转而获得的。所有这些化合物都能够抑制标记的CCK-8与大鼠胰腺腺泡和豚鼠脑膜的结合，并以不同的效力刺激大鼠胰腺腺泡释放淀粉酶。其中一些衍生物仅重现了CCK对淀粉酶释放的部分生物学反应。
