Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore

…, LH Lazarus, C Trapella, S Salvadori

Index: Salvadori, Severe; Balboni, Gianfranco; Guerrini, Remo; Tomatis, Roberto; Bianchi, Clementina; Bryant, Sharon D.; Cooper, Peter S.; Lazarus, Lawrence H. Journal of Medicinal Chemistry, 1997 , vol. 40, # 19 p. 3100 - 3108

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Citation Number: 26

Abstract

Substitution of Gly with side-chain-protected or unprotected Lys in lead compounds containing the opioid pharmacophore Dmt-Tic [H-Dmt-Tic-Gly-NH-CH2-Ph, μ agonist/δ antagonist; H-Dmt-Tic-Gly-NH-Ph, μ agonist/δ agonist; and H-Dmt-Tic-NH-CH2-Bid, δ agonist (Bid= 1 H-benzimidazole-2-yl)] yielded a new series of compounds endowed with distinct pharmacological activities. Compounds (1-10) included high δ-(K i δ= 0.068-0.64 ...