In order to study the structure-activity relationships of natural opioid deltorphins (H-Tyr-D-Met-Phe-His-Leu- Met-Asp-NH2 and H-Tyr-D-Ala-Phe-Asp[or Glu]-Val-Val-Gly-NH2), 15 analogues were synthesized by the solution method. Their activities were determined in binding studies based on displacement of μ- and δ-receptor selective radiolabels from rat brain membranes and in two bioassays, using guinea pig ileum and mouse vas deferens. The obtained data indicate that the high δ-selectivity of deltorphins can be due to the constitution/conformation of the C-terminal part and, at least in part, to preselection by charge. © 1991, American Chemical Society. All rights reserved.
Synthesis and structure activity relationships of delthorphine analogues
SALVADORI, Severo;MARASTONI, Mauro;BOREA, Pier Andrea;MORARI, Michele;TOMATIS, Roberto
1991
Abstract
In order to study the structure-activity relationships of natural opioid deltorphins (H-Tyr-D-Met-Phe-His-Leu- Met-Asp-NH2 and H-Tyr-D-Ala-Phe-Asp[or Glu]-Val-Val-Gly-NH2), 15 analogues were synthesized by the solution method. Their activities were determined in binding studies based on displacement of μ- and δ-receptor selective radiolabels from rat brain membranes and in two bioassays, using guinea pig ileum and mouse vas deferens. The obtained data indicate that the high δ-selectivity of deltorphins can be due to the constitution/conformation of the C-terminal part and, at least in part, to preselection by charge. © 1991, American Chemical Society. All rights reserved.I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
