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In this paper, we investigated the structure–activity relationship of two vasopressin analogues, [Cpa1,(L‐1‐Nal)2]AVP (I) and [Cpa1,(D‐Nal)2]AVP (II) by NMR spectroscopy and molecular modeling. Both peptides exhibit antioxytocic and antipressor potency. Inversion of configuration of the residue at position 2 converted a weak antidiuretic agonist (peptide I) into a highly potent antidiuretic antagonist...
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