Collect. Czech. Chem. Commun.
1988, 53, 2599-2603
https://doi.org/10.1135/cccc19882599
The influence of certain substitutions on 1 and 2 positions of angiotensin II on biological responses
Paul Cordopatisa, Urania Beltéa, Dimitrios Theodoropoulosa, Roger Bosséb and Emanuel Escherb
a Department of Chemistry, University of Patras, Patras 26200, Greece
b Department of Pharmacology, University of Sherbrooke, Sherbrooke, Quebec J1H, 5N4, Canada
Abstract
Position 1 modified analogues of angiotensin II, as well as two analogues with additional elimination of Arg in position 2, were prepared by means of solid phase peptide synthesis. These compounds, namely [Ser1]AT, [DOPA1]AT, [Cys1]AT, [Cys(Acm)1]AT, [N-MeAib1]AT, [Aib1, Aib2]AT and [GABA1, GABA2]AT, were tested in the classical smooth-muscle assay (rabbit aorta strip) and, for binding potency, on bovine adrenal membranes and possessed a pD2 value of 7·23, 6·79, 6·43, 5·80, 6·43, and IC50(10-10 mol l-1) value of 31·6, 23·2, nd, nd, 170·0, respectively. The last two analogues were found to be totally inactive.
