Monocyclic analogues of the μ-opioid agonist 3, 8-diazabicyclo [3.2. 1] octanes: Synthesis, modeling, and activity

D Barlocco, S Villa, W Fratta, P Fadda, D Colombo…

Index: Barlocco, Daniela; Villa, Stefania; Fratta, Walter; Fadda, Paola; Colombo, Diego; Toma, Lucio Tetrahedron, 1995 , vol. 51, # 42 p. 11547 - 11556

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Abstract

Several monocyclic derivatives structurally related to the μ-opioid agonist 3-cinnamyl-8 propionyl-3, 8-diazabicyclo [3.2. 1] octane have been synthesized and tested in binding studies using the μ-selective 3H-DAMGO as ligand. Modeling studies have been performed on the same compounds in order to explain the observed lack of affinity towards μ-opioid receptors