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

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 identificat...

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Veröffentlicht in:	FEBS letters 1988-03, Vol.229 (2), p.251-255
Hauptverfasser:	Elands, Jack, Barberis, Claude, Jard, Serge, Lammek, Bernard, Manning, Maurice, Sawyer, Wilbur H., de Kloet, E.Ronald
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Arginine Vasopressin - analogs & derivatives Arginine Vasopressin - chemical synthesis Arginine Vasopressin - metabolism Arginine Vasopressin - pharmacology Biological and medical sciences Cell Membrane - metabolism Cell receptors Cell structures and functions Female Fundamental and applied biological sciences. Psychology Indicators and Reagents Iodinated vasopressin antagonist Iodine Radioisotopes Kidney - metabolism Kinetics Liver - metabolism Liver, Kidney, Uterus Molecular and cellular biology Rats Rats, Inbred Strains Receptors, Angiotensin - metabolism Receptors, Vasopressin Uterus - metabolism Vasopressin Vasopressin receptor
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Beschreibung
Zusammenfassung:	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. 125I-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.
ISSN:	0014-5793 1873-3468
DOI:	10.1016/0014-5793(88)81135-9