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The study reports on a series of novel cyclopeptides based on the structure Tyr-[d-Lys-Phe-Phe-Asp]NH2, a mixed mu and kappa opioid receptor agonist with low nanomolar affinity, in which Phe4 residue was substituted by cyclic amino acids, such as Pro or its six-membered surrogates, piperidine-2-, 3- or 4-carboxylic acids (Pip, Nip and Inp, respectively). All derivatives exhibited high mu- and moderate...
The study reports the synthesis and biological evaluation of two opioid analogs, a monomer and a dimer, obtained as products of the solid‐phase, side‐chain to side‐chain cyclization of the pentapeptide Tyr‐d‐Lys‐Phe‐Phe‐AspNH2. The binding affinities to the mu, delta, and kappa opioid receptors, as well as results obtained in a calcium mobilization functional assay are reported. Tyr‐[d‐Lys‐Phe‐Phe‐Asp]...
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