Synthesis and structure-activity relationships of deltorphins analogs
作者:Severo Salvadori、Mauro Marastoni、Gianfranco Balboni、Pier Andrea Borea、Michele Morari、Roberto Tomatis
DOI:10.1021/jm00109a019
日期:1991.5
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 mu- and delta-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 delta-selectivity of deltorphins can be due to the constitution/conformation of the C-terminal part and, at least in part, to preselection by charge.
SALVADORI, SEVERO;MARASTONI, MAURO;BALBONI, GIANFRANCO;BOREA, PIER ANDREA+, J. MED. CHEM., 34,(1991) N, C. 1656-1661
Formation constants of silver(I) complexes of some sulphur-containing dipeptides and valylvaline
作者:Anthony Q. Lyons、Leslie D. Pettit
DOI:10.1039/dt9840002305
日期:——
Formationconstants at 25 °C and I= 0.10 mol dm –3(KNO3) have been determined for the complexes of AgI with a range of nine dipeptides which incorporate side-chains containing one (glycylmethionine and methionylglycine) or two sulphur donor atoms. In the latter case dipeptides formed from amino acids of the same and of different chiralities were studied (e.g. L-methionyl-L-methionine and L-methionyl-D-methionine)