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Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors

…, M Labarre, M Gosselin, D Bellemare…

文献索引:Page; Naismith; Schmidt; Coupal; Labarre; Gosselin; Bellemare; Payza; Brown Journal of Medicinal Chemistry, 2001 ,  vol. 44,  # 15  p. 2387 - 2390

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被引用次数: 20

摘要

The design, synthesis and pharmacological evaluation of a novel class of Dmt-Tic dipeptide analogues are described. These resulting analogues bearing different C-terminal functionalities were found to bind to the human δ receptor with high affinity. One specific class of dipeptides bearing urea/thiourea functionalities showed partial to full activation of the δ receptor. Several dipeptides also showed good binding affinities with full activation ...