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American Chemical Society, Journal of Medicinal Chemistry, 15(57), p. 6861-6866, 2014

DOI: 10.1021/jm5002925

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Synthesis of Tripeptides Containing D-Trp Substituted at the Indole Ring, Assessment of Opioid Receptor Binding and in Vivo Central Antinociception

Journal article published in 2014 by Rossella De Marco, Andrea Bedini, Santi Spampinato ORCID, Luca Gentilucci
This paper is available in a repository.
This paper is available in a repository.

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Abstract

The non-cationizable 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 i.p. administration.