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Identification and biological activity of novel peptidomimetic gastrin/CCK-B receptor agonists |
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| Authors: | Graeme Semple Hamish Ryder David A. Kendrick Andrzej R. Batt Elizabeth Mathews David P. Rooker Michael Szelke Akito Nishida Keiji Miyata |
| Affiliation: | a Ferring Research Institute, Chilworth Research Centre, Chilworth, Southampton, U.K., SO16 7NP b Neuroscience & Gastrointestinal Research Laboratories, Yamanouchi Institute for Drug Discovery Research, 21, Miyukigaoka, Tsukuba, Ibaraki 305, Japan |
| Abstract: | The design, synthesis and biological activity of two novel series of compounds derived from the basic Boc-CCK-4 structure which provide potent ligands for the gastrin/CCK-B receptor is outlined. Within these series, new pseudopeptide compounds were discovered which unexpectedly were functional agonists in vivo, as shown by their ability to stimulate basal gastric acid secretion in rats, an effect which was blocked by the potent gastrin/CCK-B receptor antagonist YM022. |
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