A fluorimetric binding assay for angiotensin II and kinin receptors

Journal of Pharmacological and Toxicological Methods
Renan P MartinS I Shimuta

Abstract

Angiotensin II (AngII) and kinins (bradykinin (BK) and des-Arg9-bradykinin (DBK)), are potent agents involved in the maintenance of blood pressure and several biological activities, and their better understanding is important to produce new drugs aimed to control arterial blood pressure. Previous studies on ligand-receptor binding have been based on radioactive methods, which led us to study a new method based on the fluorimetric method. A lanthanide attached to the N-terminal segment of the peptide (AngII, BK and DBK), which produces a time-resolved-fluorescent ligand, was used in a binding test with CHO cells expressing the AT1, AT2, B1 or B2 receptors in comparison with the same cell line tested with the radioactive ligand. Our findings indicated that the non-radioactive method provided a comparable result for the angiotensin receptors. On the other hand, the kinin receptors showed a slight reduction in the binding affinity, probably due to the linkage at the N-terminal segment and/or to the lower biological stability associated to the high temperature (37°C) used for the fluorimetric method, while the radioactive one was at 4°C. We can conclude that a time-resolved fluorescence assay would provide a sensitive method as an a...Continue Reading

References

Sep 1, 1989·Naunyn-Schmiedeberg's Archives of Pharmacology·S I ShimutaD Theodoropoulos
Aug 1, 1966·Circulation Research·P A KhairallahR K Türker
Feb 1, 1974·Canadian Journal of Physiology and Pharmacology·D RegoliC Choi
Dec 1, 1995·The Journal of Biological Chemistry·K NodaS S Karnik
May 26, 1995·The Journal of Biological Chemistry·Y H FengS S Karnik
Feb 16, 2002·Methods : a Companion to Methods in Enzymology·K J Livak, T D Schmittgen
Oct 9, 2003·The Journal of Peptide Research : Official Journal of the American Peptide Society·S C MottaC R Nakaie
Apr 20, 2004·Assay and Drug Development Technologies·Heini FrangIlkka Hemmilä
Apr 13, 2007·Physiological Reviews·Laerte OliveiraAntonio C M Paiva
Jan 10, 2008·International Immunopharmacology·Edson L SantosJoão B Pesquero
Jan 10, 2008·International Immunopharmacology·Edson L SantosJoão B Pesquero
Dec 4, 2012·International Immunopharmacology·Caroline Sandén, L M Fredrik Leeb-Lundberg

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