title: Liver angiotensin II receptors in the rat: binding properties and regulation by dietary Na+ and angiotensin II.
abstract: Recent evidence suggests that angiotensin II (AII) acts on the liver via specific receptors. The aims of this study were to examine the general binding properties of these receptors in the rat and to determine the role of dietary Na+ and AII in the regulation of AII receptors. Binding of 125I-labelled Ile5-AII to liver membranes was saturable and behaved as a single class of sites with an affinity (Ka) of 2.9 l/nmol and a Hill coefficient of 0.99. Kinetic analysis of AII binding gave estimates for the rates of association and dissociation of 42 l/mumol per min and 1.5 X 10(-2)/min respectively. The binding of analogues exhibited the following order of potency: Val5-AII greater than Ile5-AII greater than AIII greater than Sar1-Ala8-AII greater than Sar1-Gly8-AII greater than AI greater than des-Asp-AI greater than C4-C8 pentapeptide greater than Phe1-Tyr8-AII greater than neurotensin greater than luteinizing hormone-releasing hormone. Binding was enhanced by Mg2+ and Ca2+ and inhibited by EDTA and the reducing agent dithiothreitol. Low dietary Na+ affected in a biphasic manner both the Ka and concentration (Ro) of liver AII receptors. Initially, Ro decreased from 25.9 +/- 3.8 (control) to 16 +/- 1.9 (S.E.M.) pmol/g tissue by 1.5 days but thereafter it rapidly increased to 47.3 +/- 8.7 pmol/g tissue (3.5 days) and remained elevated to the end of the experiment, 8.5 days later. The Ka initially increased from 2.7 +/- 0.3 (control) to 4.3 +/- 0.5 l/nmol (1.5 days) and then decreased steadily to 1.2 +/- 0.1 l/mol (8.5 days).(ABSTRACT TRUNCATED AT 250 WORDS)
authors.forename: C
authors.initials: C
authors.lastname: Sernia
authors.forename: L
authors.initials: L
authors.lastname: Sinton
authors.forename: W G
authors.initials: WG
authors.lastname: Thomas
authors.forename: W
authors.initials: W
authors.lastname: Pascoe
mesh_terms: D000804:Angiotensin II / Q000378:metabolism* / Q000494:pharmacology; D000818:Animals; D004039:Diet, Sodium-Restricted; D008099:Liver / Q000378:metabolism*; D008297:Male; D011869:Radioligand Assay; D051381:Rats; D011919:Rats, Inbred Strains; D011945:Receptors, Angiotensin / Q000187:drug effects / Q000378:metabolism*; D011956:Receptors, Cell Surface / Q000378:metabolism*; D012964:Sodium / Q000378:metabolism
chemical_list: D011945:Receptors, Angiotensin; D011956:Receptors, Cell Surface; D000804:Angiotensin II; D012964:Sodium