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125 I‐d(CH 2 ) 5 [Tyr(Me) 2 ,Tyr(NH 2 ) 9 ]AVP: Iodination and binding characteristics of a vasopressin receptor ligand
Author(s) -
Elands Jack,
Barberis Claude,
Jard Serge,
Lammek Bernard,
Manning Maurice,
Sawyer Wilbur H.,
de Kloet E.Ronald
Publication year - 1988
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(88)81135-9
Subject(s) - chemistry , vasopressin , dissociation constant , moiety , antagonist , residue (chemistry) , halogenation , stereochemistry , dissociation (chemistry) , medicinal chemistry , receptor , endocrinology , biochemistry , organic chemistry , biology
A radioiodinated vasopressin antagonist, d(CH 2 ) 5 [Tyr(Me) 2 ,Tyr(NH 2 ) 9 ]AVP has been prepared. Iodination was carried out at the phenyl moiety of the tyrosylamide residue at position 9, followed by HPLC purification. Non‐radiolabelled monoiodinated antagonist was used as a reference for identification. 125 I‐d(CH 2 ) 5 [Tyr(Me) 2 ,Tyr(NH 2 ) 9 ]AVP binding appeared to take place with a dissociation constant of 0.28±0.09 nM ( K d ±SD) to V 1 vasopressin receptors on rat liver membranes.