super(125)I-d(CH sub(2)) sub(5)(Tyr(Me) super(2), Tyr(NH sub(2)) super(9))AVP: Iodination and binding characteristics of a vasopressin receptor ligand

A radioiodinated vasopressin antagonist, d(CH sub(2)) sub(5)(Tyr(Me) super(2), Tyr(NH sub(2)) super(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...

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Veröffentlicht in:FEBS letters 1988-01, Vol.229 (2), p.251-255
Hauptverfasser: Elands, J, Barberis, C, Jard, S, Lammek, B, Manning, M, Sawyer, W H, de Kloet, ER
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Sprache:eng
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Zusammenfassung:A radioiodinated vasopressin antagonist, d(CH sub(2)) sub(5)(Tyr(Me) super(2), Tyr(NH sub(2)) super(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. super(125)I-d(CH sub(2)) sub(5) (Tyr(Me) super(2), Tyr(NH sub(2)) super(9))AVP binding appeared to take place with a dissociation constant of 0.28 plus or minus 0.09 nM (K sub(d) plus or minus SD) to V sub(1) vasopressin receptors on rat liver membranes.
ISSN:0014-5793