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Title: Interaction of a vasopressin antagonist with vasopressin receptors in the septum of the rat brain

Abstract

The ability of d(CH2)5-Tyr(Me)-arginine-8-vasopressin, an antagonist of peripheral pressoric (V1-type) vasopressin receptors, to label vasopressin binding sites in the septum of the rat brain was evaluated. Using crude membrane preparations from the septum, /sup 3/H-arginine-8-vasopressin (AVP) specifically labels a single class of binding sites with a Kd of 2.9 nM and maximum binding site concentration of 19.8 fmole/mg protein. /sup 3/H-Antag also labels a single class of membrane sites but with higher affinity (Kd = 0.47 nM) and lower capacity (10.1 fmole/mg protein) than /sup 3/H-AVP. The rank order of potency of various competitor peptides for /sup 3/H-AVP and /sup 3/H-Antag binding was similar. Oxytocin was 100-1,000 fold less potent than AVP in competing for binding with both ligands. /sup 3/H-AVP and /sup 3/H-Antag showed similar labeling patterns when incubated with septal tissue slices. Unlabeled Antag also effectively antagonized vasopressin-stimulated phosphatidylinositol hydrolysis in septal tissue slices.

Authors:
; ; ; ; ;
Publication Date:
Research Org.:
Veterans Administration Medical Center, Seattle, WA (USA)
OSTI Identifier:
6354119
Resource Type:
Journal Article
Resource Relation:
Journal Name: Synapse; (United States); Journal Volume: 2:3
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES; RECEPTORS; LABELLING; VASOPRESSIN; AUTORADIOGRAPHY; BIOCHEMICAL REACTION KINETICS; BRAIN; CELL MEMBRANES; IN VITRO; RATS; TRITIUM COMPOUNDS; ANIMALS; BODY; CELL CONSTITUENTS; CENTRAL NERVOUS SYSTEM; HORMONES; KINETICS; LABELLED COMPOUNDS; MAMMALS; MEMBRANE PROTEINS; MEMBRANES; NERVOUS SYSTEM; ORGANIC COMPOUNDS; ORGANS; PEPTIDE HORMONES; PITUITARY HORMONES; PROTEINS; REACTION KINETICS; RODENTS; VERTEBRATES; 550201* - Biochemistry- Tracer Techniques

Citation Formats

Dorsa, D.M., Brot, M.D., Shewey, L.M., Meyers, K.M., Szot, P., and Miller, M.A.. Interaction of a vasopressin antagonist with vasopressin receptors in the septum of the rat brain. United States: N. p., 1988. Web. doi:10.1002/syn.890020306.
Dorsa, D.M., Brot, M.D., Shewey, L.M., Meyers, K.M., Szot, P., & Miller, M.A.. Interaction of a vasopressin antagonist with vasopressin receptors in the septum of the rat brain. United States. doi:10.1002/syn.890020306.
Dorsa, D.M., Brot, M.D., Shewey, L.M., Meyers, K.M., Szot, P., and Miller, M.A.. Fri . "Interaction of a vasopressin antagonist with vasopressin receptors in the septum of the rat brain". United States. doi:10.1002/syn.890020306.
@article{osti_6354119,
title = {Interaction of a vasopressin antagonist with vasopressin receptors in the septum of the rat brain},
author = {Dorsa, D.M. and Brot, M.D. and Shewey, L.M. and Meyers, K.M. and Szot, P. and Miller, M.A.},
abstractNote = {The ability of d(CH2)5-Tyr(Me)-arginine-8-vasopressin, an antagonist of peripheral pressoric (V1-type) vasopressin receptors, to label vasopressin binding sites in the septum of the rat brain was evaluated. Using crude membrane preparations from the septum, /sup 3/H-arginine-8-vasopressin (AVP) specifically labels a single class of binding sites with a Kd of 2.9 nM and maximum binding site concentration of 19.8 fmole/mg protein. /sup 3/H-Antag also labels a single class of membrane sites but with higher affinity (Kd = 0.47 nM) and lower capacity (10.1 fmole/mg protein) than /sup 3/H-AVP. The rank order of potency of various competitor peptides for /sup 3/H-AVP and /sup 3/H-Antag binding was similar. Oxytocin was 100-1,000 fold less potent than AVP in competing for binding with both ligands. /sup 3/H-AVP and /sup 3/H-Antag showed similar labeling patterns when incubated with septal tissue slices. Unlabeled Antag also effectively antagonized vasopressin-stimulated phosphatidylinositol hydrolysis in septal tissue slices.},
doi = {10.1002/syn.890020306},
journal = {Synapse; (United States)},
number = ,
volume = 2:3,
place = {United States},
year = {Fri Jan 01 00:00:00 EST 1988},
month = {Fri Jan 01 00:00:00 EST 1988}
}