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Synthesis and evaluation of the affinity toward μ-opioid receptors of atypical, lipophilic ligands based on the sequence c [-Tyr-Pro-Trp-Phe-Gly-]

…, M Calienni, AR Qasem, S Spampinato

文献索引:Cardillo, Giuliana; Gentilucci, Luca; Tolomelli, Alessandra; Qasem, Ahmed R; Spampinato, Santi; Calienni, Maria Organic and biomolecular chemistry, 2003 , vol. 1, # 17 p. 3010 - 3014

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被引用次数: 41

摘要

An ultimate and general model describing the interaction between opioid ligands and μ- opioid receptors is not available yet, so the mode of action of atypical peptide analogues or peptidomimetics is worthy of investigation. In this context, the peptide c [-Tyr-d-Pro-d-Trp- Phe-Gly-] was observed to act as an agonist toward μ-opioid receptors with appreciable potency, albeit deprived of a protonable nitrogen. This compound was synthesized as a ...