B Lammek, E Konieczna, T Wierzba, Y X Wang, H Gavras
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Synthesis and some pharmacological properties of new V1/V2 antagonists of arginine-vasopressin with structural changes at their N-terminals.
In an effort to develop more effective and selective V2-antagonists of arginine-vasopressin (AVP) we designed and synthesized four new analogs of this hormone. The peptides were designed in order to explore how the combination of modification of thioacids occupying position 1 and substitutions of positions 2 and 4 by D-Phe and Ile respectively, will influence their antagonistic properties. Three of the reported analogs are moderately potent V1/V2 antagonists.
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