Characterization of a novel, linear radioiodinated vasopressin antagonist: an excellent radioligand for vasopressin V1a receptors

Details

Serval ID
serval:BIB_10199294EBE4
Type
Article: article from journal or magazin.
Collection
Publications
Institution
Title
Characterization of a novel, linear radioiodinated vasopressin antagonist: an excellent radioligand for vasopressin V1a receptors
Journal
Neuroendocrinology
Author(s)
Barbeis  C., Balestre  M. N., Jard  S., Tribollet  E., Arsenijevic  Y., Dreifuss  J. J., Bankowski  K., Manning  M., Chan  W. Y., Schlosser  S. S., Holsboer  F., Elands  J.
ISSN
0028-3835 (Print)
Publication state
Published
Issued date
08/1995
Volume
62
Number
2
Pages
135-46
Notes
Journal Article Research Support, Non-U.S. Gov't Research Support, U.S. Gov't, P.H.S. --- Old month value: Aug
Abstract
We report on the pharmacological properties of a potent and selective linear vasopressin (AVP) V1a receptor antagonist HO-Phenylacetyl1-D-Tyr(Me)2-Phe3-Gln4-Asn5-Arg6-Pro7-Arg8-NH2 (HO-LVA). Iodinated on the phenolic substituent at position 1, [125I]-HO-LVA displayed the highest affinity for rat liver V1a receptors (8 pM) ever reported. Furthermore, affinities of HO-LVA and I-HO-LVA for V1b, V2 and oxytocin (OT) receptors was 400- to 1,000-fold lower than for V1a receptors, rendering it a highly selective ligand. Both HO-LVA and its iodinated derivative are V1 antagonists, they potently inhibited AVP-induced inositol-phosphate accumulation in WRK1 cells, and also, although with a much lower potency, the AVP-induced ACTH release from freshly prepared pituitary cells. Using autoradiography [125I]-HO-LVA appeared to be the first radioligand to successfully identify and localize the presence of V1a receptors in rat liver and blood vessel walls. Moreover, several new brain regions expressing V1a receptors could be identified, in addition to those brain regions that were previously identified with other radiolabelled AVP analogues.
Keywords
Adrenocorticotropic Hormone/secretion Amino Acid Sequence Animals Arginine Vasopressin/pharmacology Autoradiography Cell Membrane/metabolism Female Inositol Phosphates/metabolism *Iodine Radioisotopes Liver/metabolism Mammary Neoplasms, Experimental Molecular Sequence Data Oligopeptides/*metabolism/pharmacology Pituitary Gland/drug effects/secretion Rats Rats, Wistar Receptors, Oxytocin/metabolism Receptors, Vasopressin/analysis/*metabolism Tissue Distribution Tumor Cells, Cultured Vasopressins/*antagonists & inhibitors
Pubmed
Web of science
Create date
28/01/2008 12:31
Last modification date
20/08/2019 12:36
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