Abstract
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.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Antidiuretic Hormone Receptor Antagonists*
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Arginine Vasopressin / analogs & derivatives*
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Arginine Vasopressin / chemical synthesis
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Arginine Vasopressin / chemistry
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Arginine Vasopressin / pharmacology
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Autoradiography
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DNA / biosynthesis
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Diuresis / drug effects
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Humans
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Inosine Triphosphate / metabolism
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Iodine Radioisotopes
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Rats
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Receptors, Oxytocin / drug effects
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Receptors, Oxytocin / metabolism
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Receptors, Vasopressin / biosynthesis
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Receptors, Vasopressin / metabolism
Substances
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Antidiuretic Hormone Receptor Antagonists
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Iodine Radioisotopes
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Receptors, Oxytocin
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Receptors, Vasopressin
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argipressin, d(CH2)5-O-ethyl-Tyr(2)-Val(4)-Tyr-NH2(9)-
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Arginine Vasopressin
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Inosine Triphosphate
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DNA