A non-radioactive method for angiotensin II receptor binding studies using the rat liver

Akhavan, M.M. and Ebrahimi, S.A. and Mahmoudian, M. (2006) A non-radioactive method for angiotensin II receptor binding studies using the rat liver. Journal of Pharmacological and Toxicological Methods, 53 (3). pp. 206-214.

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Abstract

Introduction: A new non-radioactive method based on competitive ELISA has been developed for binding studies on angiotensin II (Ang II) receptors. Method: Rat liver membrane was used as the source of angiotensin receptors and FITC-angiotensin II (FITC-Ang II) was used as the labeled ligand with an affinity similar to unlabeled Ang II. The effects of different concentrations of Ang II, losartan, CGP-42112A and saralasin were studied on FITC-Ang II binding. Results: The Ki values for Ang II, losartan and CGP-42112A were calculated as 0.52 ± 0.22 nM, 6 ± 3 nM and 0.15 ± 0.07 nM, respectively. Saralasin inhibited the binding of labeled ligand biphasically, revealing two different populations of Ang receptor with different affinities for saralasin. About 74 of the binding sites were more sensitive to saralasin with a Ki value of 0.32 ± 0.04 nM while saralasin showed a Ki value of 2.7 ± 0.8 nM for the remaining binding sites. Discussion: The competitive ELISA method developed in this work yields Ki values for angiotensin antagonists similar to those obtained by others using radiolabeled ligands. The simplicity of this method makes it a suitable alternative to radioligand studies for routine analysis of interaction of drugs with angiotensin receptors. © 2005 Elsevier Inc. All rights reserved.

Item Type: Article
Additional Information: cited By 3
Uncontrolled Keywords: angiotensin 2 receptor; angiotensin antagonist; angiotensin II; fluorescein isothiocyanate; losartan; nicotinoyltyrosyl(n benzyloxycarbonylarginyl)lysylhistidylprolylisoleucine; saralasin, animal tissue; article; binding affinity; concentration (parameters); controlled study; drug binding site; drug receptor binding; enzyme linked immunosorbent assay; ligand binding; liver membrane; male; nonhuman; radioassay; rat; receptor sensitivity, Angiotensin II; Animals; Binding Sites; Binding, Competitive; Biological Assay; Cell Membrane; Dose-Response Relationship, Drug; Enzyme-Linked Immunosorbent Assay; Fluorescein-5-isothiocyanate; Fluorescent Antibody Technique, Indirect; Fluorescent Dyes; Kinetics; Ligands; Liver; Losartan; Male; Models, Immunological; Oligopeptides; Rats; Rats, Wistar; Receptors, Angiotensin; Saralasin; Vasoconstrictor Agents; Vasodilator Agents, Animalia
Depositing User: EPrints System Admin
Date Deposited: 19 Jul 2017 10:13
Last Modified: 19 Jul 2017 10:13
URI: http://eprints.iums.ac.ir/id/eprint/56

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