American Chemical Society, Journal of Medicinal Chemistry, 15(57), p. 6861-6866, 2014
DOI: 10.1021/jm5002925
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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.