jm5002925_si_001.pdf (538.82 kB)
Synthesis of Tripeptides Containing d‑Trp Substituted at the Indole Ring, Assessment of Opioid Receptor Binding and in Vivo Central Antinociception
journal contribution
posted on 2014-08-14, 00:00 authored by Rossella De Marco, Andrea Bedini, Santi Spampinato, Luca GentilucciThe
noncationizable tripeptide Ac-d-Trp-Phe-GlyNH2 was recently proposed as a novel minimal recognition motif
for μ-opioid receptor. The introduction of different substituents
(methyl, halogens, nitro, etc.) at the indole of d-Trp significantly
influenced receptor affinities and resulted in serum stability and
in a measurable effect on central antinociception in mice after ip
administration.