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  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.

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

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 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.

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Language(s): eng - English
 Dates: 1986-08-111986-06-092005-03-031986-12-01
 Publication Status: Published in print
 Pages: 8
 Publishing info: -
 Table of Contents: -
 Rev. Type: Peer
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Title: European Journal of Biochemistry
Source Genre: Journal
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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