Synthesis and binding activity of endomorphin-1 analogues containing β-amino acids

…, L Gentilucci, P Melchiorre, S Spampinato

Index: Cardillo, Giuliana; Gentilucci, Luca; Melchiorre, Paolo; Spampinato, Santi Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 24 p. 2755 - 2758

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Citation Number: 61

Abstract

Endomorphin-1 (Tyr-Pro-Trp-PheNH2) has been proposed as the most potent endogenous ligand of the μ-opioid receptors. In this paper, we describe the synthesis of some endomorphin-1 based tetrapeptides in which a residue of the sequence Tyr-Pro-Trp- PheNH2 is replaced by the corresponding β-isomer. These novel peptides showed different affinities for the opioid receptors labeled with [3H]-DAMGO in rat brain membranes, ...