125I-labelled d(CH2)5[Tyr(Me)2,Thr4,Tyr-NH29]OVT: a selective oxytocin receptor ligand
Abstract
An oxytocic antagonist, [1-(beta-mercapto-beta, beta-cyclopentamethylenepropionic acid,2-O-methyltyrosine,4-threonine, 8-ornithine,9-tyrosylamide]vasotocin (d(CH2)5[Tyr(Me)2, Thr4,Tyr-NH2(9)]OVT [corrected], was monoiodinated at the phenyl moiety of the tyrosylamide residue at position 9. 125I-labelling was performed with 1,3,4,6-tetrachloro-3 alpha,6 alpha-diphenyl-glycoluril. Iodination resulted in an increased affinity for rat uterine oxytocin receptors. A considerably lower affinity for rat vascular V1- and renal V2-receptors was found, resulting in a highly specific oxytocin receptor ligand. 125I-labelled d(CH2)5[Tyr(Me)2,Thr4,Tyr-NH2(9)]OVT [corrected] was demonstrated to bind selectively to one population of binding sites in rat uterus and ventral hippocampal membrane preparations. Dissociation constants ranged between 0.03 and 0.06 nM. After 3 days of exposure autoradiography revealed binding in regions known to contain oxytocin receptors as well as labelling in some new regions, while no binding was found in the lateral septum, a structure containing mainly [8-arginine]vasopressin receptors. The high specific radioactivity of 125I-labelling allowed important reductions in membrane protein amount, gain in precision of binding analysis as well as considerably lower exposure times for autoradiography.
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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 [15]
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- Authors
- Elands, J., Barberis, C., Jard, S., Tribollet, E., Dreifuss, J.-J., Bankowski, K., Manning, M., & Sawyer, W. H.
- Affiliations
- Centre National de la Recherche Scientifique (FR)
- University of Toledo Medical Center (US)
- Columbia University (US)
- Corresponding author
- Barberis, Claude
- Venue
- European Journal of Pharmacology
- Publisher
- Elsevier BV
- Published
- 1988-03
- Volume
- 147
- Issue
- 2
- Pages
- 197-207
- ISSN
- 0014-2999 (ISSN-L)
- OpenAlex
- W2070821979
- Cited by
- 245
- References
- 33
- Citations by year
- 2026: 1 · 2024: 2 · 2023: 3 · 2021: 5 · 2020: 2 · 2019: 4 · 2018: 3 · 2017: 1 · 2016: 4 · 2015: 1 · 2014: 1 · 2013: 3 · 2012: 3
- FWCI
- 27.26
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- European Journal of Pharmacology (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Institute of General Medical Sciences (GM25280)
- National Institute of Diabetes and Digestive and Kidney Diseases (DK-01940)
- Topics
- Social Sciences › Psychology › Social Psychology › Neuroendocrine regulation and behavior
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
- Health Sciences › Medicine › Surgery › Cardiovascular, Neuropeptides, and Oxidative Stress Research
- Keywords
- oxytocin receptor, arginine vasotocin, iodine-125 labeling, iodination, receptor antagonists, receptor selectivity, ventral hippocampus, binding affinity, autoradiography
- MeSH terms
- Animals, Autoradiography, Brain Chemistry, Chromatography, High Pressure Liquid, Female, Iodine Radioisotopes, Kidney, Ligands, Liver, Oxytocin, Rats, Inbred Strains, Receptors, Angiotensin, Uterus, Receptors, Oxytocin, Rats, In Vitro Techniques
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