Abstract The diazatricyclodecane derivatives belong to a novel class of δ opioid receptor agonists, conformationally restricted analogs of SNC‐80. To support further investigation on the potential use of this class of δ opioid receptor agonists in humans, synthesis and chemical characterization of three tricyclic compounds of this class, designated as 3–4 ‐ 5 , was carried out. Moreover, drug metabolism of the same compounds was investigated using human liver microsomes. Being drug candidates chiral compounds, they were also evaluated in terms of stereoisomers presence in the drug substances. Pharmacokinetic profiles and kinetic parameters of compound 3 and compound 4 and Michaelis parameters of compound 3 were determined. Remaining percentages of the parent drug versus time were analyzed. Results indicated that the examined derivatives display good in vitro metabolic stability.