125I-d(CH2)5[Tyr(Me)2, Tyr(NH2)9]AVP: iodination and binding characteristics of a vasopressin receptor ligand

FEBS Lett. 1988 Mar 14;229(2):251-5. doi: 10.1016/0014-5793(88)81135-9.

Abstract

A radioiodinated vasopressin antagonist, d(CH2)5[Tyr(NH2)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(CH2)5[Tyr(Me)2, Tyr(NH2)9]AVP binding appeared to take place with a dissociation constant of 0.28 +/- 0.09 nM (Kd +/- SD) to V1 vasopressin receptors on rat liver membranes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Arginine Vasopressin / analogs & derivatives*
  • Arginine Vasopressin / chemical synthesis
  • Arginine Vasopressin / metabolism*
  • Arginine Vasopressin / pharmacology
  • Cell Membrane / metabolism
  • Female
  • Indicators and Reagents
  • Iodine Radioisotopes
  • Kidney / metabolism
  • Kinetics
  • Liver / metabolism
  • Rats
  • Rats, Inbred Strains
  • Receptors, Angiotensin / metabolism*
  • Receptors, Vasopressin
  • Uterus / metabolism

Substances

  • Indicators and Reagents
  • Iodine Radioisotopes
  • Receptors, Angiotensin
  • Receptors, Vasopressin
  • Arginine Vasopressin
  • argipressin, beta mercapto-beta,beta-cyclopentamethylenepropionic acid(1)-O-methyl-Tyr(2)-TyrNH2(9)-