Novel ligands rationally designed for characterizing I-2-imidazoline binding sites nature and functions

摘要

The study of two series of 2-aryl-ethylen-imidazolines 3-7 and 8-12 inspired by I-2-IBS ligands phenyzoline (1) and diphenyzoline (2), respectively, confirmed the interesting "positive" or "negative" morphine analgesia modulation displayed by their corresponding leads and demonstrated that these effects might be correlated with morphine tolerance and dependence, respectively. By comparative examination of rationally designed compounds, some analogies between binding site cavity of I-2-IBS proteins and alpha(2C)-adrenoreceptor emerged.