125I‐d(CH2)5[Tyr(Me)2,Tyr(NH2)9]AVP: Iodination and binding characteristics of a vasopressin receptor ligand
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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.
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Highly selective radiolabelled peptide analogues for oxytocin receptor and vasopressin receptor 1a binding were later developed for rodent brain tissue.
“Later, highly selective radiolabelled peptide analogues for OXTR and AVPR1a binding were developed for use in rodent brain tissue (15,16).”
From Comparative Perspectives on Oxytocin and Vasopressin Receptor Research in Rodents and Primates: Translational Implications (2016) · cites this paper as [16]
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References 10 · Cited by 28
- Authors
- Elands, J., Barberis, C., Jard, S., Lammek, B., Manning, M., Sawyer, W. H., & de Kloet, E. R.
- Affiliations
- Centre National de la Recherche Scientifique (FR)
- Columbia University (US)
- Corresponding author
- Jard, Serge
- Venue
- FEBS Letters
- Publisher
- Wiley
- Published
- 1988-03-14
- Volume
- 229
- Issue
- 2
- Pages
- 251-255
- ISSN
- 0014-5793 (ISSN-L)
- 1873-3468
- OpenAlex
- W2026534787
- Cited by
- 28
- References
- 10
- Citations by year
- 2021: 2 · 2018: 1 · 2016: 2 · 2015: 1
- FWCI
- 0.55
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- FEBS Letters (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Radiopharmaceutical Chemistry and Applications
- Health Sciences › Medicine › Surgery › Cardiovascular, Neuropeptides, and Oxidative Stress Research
- Keywords
- vasopressin receptor, vasopressin receptor antagonists, radioiodination, iodine-125, receptor binding, dissociation constant, rat liver membranes, peptide ligands
- MeSH terms
- Animals, Arginine Vasopressin, Cell Membrane, Female, Indicators and Reagents, Iodine Radioisotopes, Kidney, Kinetics, Liver, Rats, Inbred Strains, Receptors, Angiotensin, Uterus, Receptors, Vasopressin, Rats
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