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. 1990 May;35(5):441-51.
doi: 10.1111/j.1399-3011.1990.tb00071.x.

Synthesis of cyclic analogues of cholecystokinin highly selective for central receptors

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Synthesis of cyclic analogues of cholecystokinin highly selective for central receptors

M Rodriguez et al. Int J Pept Protein Res. 1990 May.

Abstract

Cyclic CCK analogues in which positions 28 and 31 have been replaced by lysine residues and whose side chains are bridged by a succinic moiety, were synthesized. They were tested for their ability to inhibit the binding of 125I-BH-CCK-8 to isolated rat pancreatic acini and to guinea pig brain membranes. These cyclic CCK-analogues were compared to the potent CCK analogue Boc-[Nle28,31]-CCK-7 and to Boc-Trp-Leu-Asp-Phe-NH2, analogue of CCK-4. These cyclic compounds appeared to be highly selective for central CCK receptors.

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