title: Angiotensin II binding sites in the heart of Scyliorhinus canicula: an autoradiographic study.
abstract: Dogfish (125)I [Asn(1), Pro(3), Ile(5)] angiotensin II ((125)I dfANG II) was used to establish the specific binding patterns of the different cardiac regions of the elasmobranch Scyliorhinus canicula by in vitro autoradiography. In the ventricular myocardium Scatchard analysis of saturation and displacement binding data revealed two classes of high- and low-affinity dfANG II binding sites (K(d) = 53 +/- 10 and 1300 +/- 900 pM). Two classes of dfANG II binding sites were also detected in the atrium (K(d) = 47 +/- 13 and 4690 +/- 930 pM) and in the outer layer of the conus arteriosus (K(d) = 16 +/- 9 and 398 +/- 83 pM). Conversely, the ventricular endocardium and the inner conal layer were characterized by a single class of dfANG II binding sites with affinity values of 48 +/- 11 and 106 +/- 3.3 pM, respectively. Competition experiments with either cold dfANG II or CV11974 or CGP42112 (specific ligands for mammalian AT(1) and AT(2) receptors, respectively) demonstrated a prevalence of CGP42112-selective dfANG II binding sites in both the inner and the outer conal layers. In the atrium, the ventricular myocardium, and the outer conal layer, dfANG II high-affinity binding sites poorly discriminated among the cold ligands. These results suggest that the dogfish heart may be a target organ of ANG II with distinct ANG II receptor subtype distributions.
authors.affiliation: Department of Pharmaco-Biology, University of Calabria, 87030 Arcavacata di Rende, CS, Italy.
authors.forename: M C
authors.initials: MC
authors.lastname: Cerra
authors.forename: M L
authors.initials: ML
authors.lastname: Tierney
authors.forename: Y
authors.initials: Y
authors.lastname: Takei
authors.forename: N
authors.initials: N
authors.lastname: Hazon
authors.forename: B
authors.initials: B
authors.lastname: Tota
mesh_terms: D000804:Angiotensin II / Q000378:metabolism*; D057911:Angiotensin Receptor Antagonists; D000818:Animals; D001345:Autoradiography; D001562:Benzimidazoles / Q000494:pharmacology; D001665:Binding Sites / Q000187:drug effects; D001713:Biphenyl Compounds; D004284:Dogfish / Q000502:physiology*; D004699:Endocardium / Q000378:metabolism; D006325:Heart Atria / Q000378:metabolism; D007457:Iodine Radioisotopes; D009206:Myocardium / Q000378:metabolism*; D009842:Oligopeptides / Q000494:pharmacology; D011945:Receptors, Angiotensin / Q000378:metabolism*; D013777:Tetrazoles / Q000494:pharmacology
chemical_list: D057911:Angiotensin Receptor Antagonists; D001562:Benzimidazoles; D001713:Biphenyl Compounds; D007457:Iodine Radioisotopes; D009842:Oligopeptides; D011945:Receptors, Angiotensin; D013777:Tetrazoles; D000804:Angiotensin II; C060894:CGP 42112A; C081643:candesartan