Pseudopeptide CCK-4 analogues incorporating the Ψ[CH(CN)NH] peptide bond surrogate

Article abstract of DOI:10.1016/S0960-894X(97)00107-8

The synthesis, binding to CCK receptors, and in vitro functional activity of pseudopeptide CCK-4 analogues incorporating the (R) or (S) Ψ[CH(CN)NH] peptide bond surrogate at the Nle³¹-Asp³² or Trp³⁰-Nle³¹ bonds are described. Z-TrpΨ[(S)CH(CN)NH]Nle-Asp-Phe-NH₂ retained the high CCK-B receptor binding affinity of Boc-[Nle³¹]-CCK-4, and was a potent and selective CCK-B antagonist in the isolated guinea pig ileum.