English
 
Help Privacy Policy Disclaimer
  Advanced SearchBrowse

Item

ITEM ACTIONSEXPORT
  Iodinated photoreactive vasopressin antagonists: labelling of hepatic vasopressin receptor subunits

Fahrenholz, F., Kojro, E., Müller, M., Boer, R., Löhr, R., & Grzonka, Z. (1986). Iodinated photoreactive vasopressin antagonists: labelling of hepatic vasopressin receptor subunits. European Journal of Biochemistry, 161(2), 321-328. doi:10.1111/j.1432-1033.1986.tb10450.x.

Item is

Files

show Files

Locators

show

Creators

show
hide
 Creators:
Fahrenholz, Falk1, Author           
Kojro, Elzbieta1, Author           
Müller, Michael1, Author           
Boer, Rainer1, Author           
Löhr, Reinhold1, Author           
Grzonka, Zbigniew2, Author
Affiliations:
1Department of Physical Chemistry, Max Planck Institute of Biophysics, Max Planck Society, ou_3264819              
2Institute of Chemistry, University of Gdansk, Poland, ou_persistent22              

Content

show
hide
Free keywords: -
 Abstract: To identify and characterize V1 vasopressin receptors, photoreactive antagonists of the glycogenolytic and vasoconstrictor activity of vasopressin have been synthesized. The following analogues with 3‐mercapto‐ 3,3‐cyclopentamethylene‐propionic acid (Mca) and N‐methylalanine (MeAla) in position 1 and 7 of vasopressin (VP) were effective V1 antagonists: [Mca1,D‐Tyr2,MeAla7,Lys8]VP (l), [Mca1,MeAla7,Arg8,Lys9]VP (2), [Mca1,MeAla7,Arg8,d‐Lys9]VP (3). Introduction of the photoreactive 4‐azidophenylamidino group into the side‐ chain of Lyss8 in analogue 1 or into Lys9 in analogues 2 and 3 increased the potency (for analogue 1 a tenfold increase in the antiglycogenolytic effect and a fivefold increase in the antivasopressor effect) and binding affinity for the rat hepatic V1 receptor. Mono‐iodination at Tyr2 with 125I resulted in photoreactive antagonists of high specific radioactivity, which had roughly the same binding affinity as vasopressin for the rat hepatic V1 receptor (Kd= 0.9—1.8 nM).

In photoaffinity labelling experiments with purified rat liver membranes, containing 2–3 pmol V1 receptor/ mg protein, the analogues labelled specifically two proteins with the relative molecular masses (Mr) of 30000 and 38 000. These results and the results of a recent study using 3H‐labelled photoreactive vasopressin agonists [Boer, R. and Fahrenholz, F. (1985) J. Bid. Chem. 260, 15051 ‐ 150541 provide evidence that both vasopressin agonists and antagonists can interact with the same two subunits of the heterodimeric hepatic V1 receptor. Furthermore the radioiodinated photoreactive V1 antagonists should be helpful to identify V1 receptor proteins in membranes of other cell types.

Details

show
hide
Language(s): eng - English
 Dates: 1986-08-111986-06-092005-03-031986-12-01
 Publication Status: Issued
 Pages: 8
 Publishing info: -
 Table of Contents: -
 Rev. Type: Peer
 Degree: -

Event

show

Legal Case

show

Project information

show

Source 1

show
hide
Title: European Journal of Biochemistry
Source Genre: Journal
 Creator(s):
Affiliations:
Publ. Info: Berlin : Published by Springer-Verlag on behalf of the Federation of European Biochemical Societies
Pages: - Volume / Issue: 161 (2) Sequence Number: - Start / End Page: 321 - 328 Identifier: ISSN: 0014-2956
CoNE: https://pure.mpg.de/cone/journals/resource/111097776606040