Journal of Medicinal Chemistry 2001-07-19

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

D Pagé, A Naismith, R Schmidt, M Coupal, M Labarre, M Gosselin, D Bellemare, K Payza, W Brown

Index: J. Med. Chem. 44(15) , 2387-90, (2001)

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Abstract

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 delta receptor with high affinity. One specific class of dipeptides bearing urea/thiourea functionalities showed partial to full activation of the delta receptor. Several dipeptides also showed good binding affinities with full activation of the human kappa receptor, a novel property for those ligands.