G. Semple et al., IDENTIFICATION AND BIOLOGICAL-ACTIVITY OF NOVEL PEPTIDOMIMETIC GASTRIN CCK-B RECEPTOR AGONISTS/, Bioorganic & medicinal chemistry letters, 6(24), 1996, pp. 2971-2976
The design, synthesis and biological activity of two novel series of c
ompounds derived from the basic Boc-CCK-4 structure which provide pote
nt ligands for the gastrin/CCK-B receptor is outlined. Within these se
ries, new pseudopeptide compounds were discovered which unexpectedly w
ere functional agonists in vivo, as shown by their ability to stimulat
e basal gastric acid secretion in rats, an effect which was blocked by
the potent gastrin/CCK-B receptor antagonist YM022. Copyright (C) 199
6 Elsevier Science Ltd