作者: Andree Turcotte , Jean-Marc Lalonde , Serge St-Pierre , Simon Lemaire
DOI: 10.1111/J.1399-3011.1984.TB02732.X
关键词:
摘要: Dynorphin-(1–13) (Dyn-(1–13)) and its analogs substituted by single introduction of Ala in positions 1–11 were synthesized the solid-phase method purified high pressure liquid chromatography. Relative potencies synthetic compounds determined their ability to inhibit electrically-evoked contractions guinea pig ileum (GPI) mouse vas deferens (MVD) compete with [3H]-etorphine for opiate receptors rat brain homogenates. Introduction 1 4 Dyn-(1–13) provoked most important decreases activity molecule three assays (relative potency 0.2% or less). Substitution 2 5, but not 3, also severely decreased peptide smooth muscle preparations (0.6–5.0% activity). However, receptor binding assay was less sensitive replacement residue position (20% activity) than that 3 5 (12% 6% relative potencies, respectively). In GPI test, other substitutions which greatly lowered seen 6, 7, 9 11, four basic residues. Among these, Arg6 Arg7 demonstrated be biological tests. Finally, Ile8 increased up 191% 900% MVD tests, respectively.