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.
This article describes a pilot study to test the adequacy of a newly developed tool for an awareness plan on the importance of properly using pharmaceuticals. The new tool consists of face-to-face interviews with adult citizens on their approach to the use of medicines and of the following data analysis with a dedicated software application. The pilot study was carried out in a sample area of Sardinia, in Italy. The data from the interviews collected anonymously and analysed in aggregate actually emphasised the critical issues and needs in the use of pharmaceuticals in the sample area involved, also encouraging communication among different actors. The pilot study revealed that the designed tool could represent a novel strategy to stimulate interchanges of information on the proper use of pharmaceuticals with a potential impact on people’s health.
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