Monocyclic Analogs of the mu-opioid Agonist 3,8-diazabicyclo-[3.2.1]octanes - Synthesis, Modeling, and Activity

Several monocyclic derivatives structurally related to the mu-opioid agonist 3-cinnamyl-8-propionyl-3,8-diazabicyclo[3.2.1]octane have been synthesized and tested in binding studies using the mu-selective H-3-DAMGO as ligand. Modeling studies have been performed on the same compounds in order to explain the observed lack of affinity towards mu-opioid receptors.