Properties of a New Radioiodinated Antagonist for Human Vasopressin V2 and V1a Receptors

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Title: Properties of a New Radioiodinated Antagonist for Human Vasopressin V2 and V1a Receptors
Authors: Ala, Youssef; Morin, Denis; Mahe, Eve; Cotte, Nathalie; Mouillac, Bernard; Jard, Serge; Barberis, Claude; Tribollet, Eliane; Dreifuss, Jean-Jacques; Sawyer, Wilbur H.; Wo, Nga Ching; Chan, W. Y.; Kolodziejczyk, Aleksandra S.; Cheng, Ling Ling; Manning, Ph.D., D.Sc., Maurice
Publisher: European Journal of Pharmacology
Date Published: July 01, 1997
Reference Number: 362
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A vasopressin receptor antagonist, [1-(beta-mercapto-beta,beta-pentamethylenepropionic acid), 2-o-ethyl-D-tyrosine, 4-valine, 9-tyrosylamide] arginine vasopressin (d(CH2)5[o-ethyl-D-Tyr2,Val4,Tyr-NH9(2)]AVP), has been prepared. This antagonist is a potent antiantidiuretic, antivasopressor and antioxytocic peptide with pA2 values of 7.69-7.94 and affinities of 1.12-11.0 nM. When radioiodinated at the phenyl moiety of the tyrosylamide residue at position 9, this peptide was demonstrated to bind to vasopressin V2 and V1a receptors with a dissociation constant of 0.22-0.75 nM. This ligand is a good tool for further studies on human vasopressin V2 receptor localization and characterization, when used in combination with a selective vasopressin V1a ligand.