[摘要]：The goal of the present study was to modulate the receptor interaction properties of known a2-adrenoreceptor (AR) antagonists to obtain novel a2-AR agonists with desirable subtype selectivity. Therefore, a Ph group or one of its bioisosteres or aliph. moieties with similar steric hindrance were introduced into the arom. ring of the antagonist lead basic structure. The functional properties of the novel compds. allowed our previous observations to be confirmed. The high efficacy of 7, 12, and 13 as a2-AR agonists and the significant a2C-AR subtype selective activation displayed by 11 and 15 demonstrated that favorable interactions to induce a2-AR activation were formed between the pendant groups of the ligands and the arom. cluster present in transmembrane domain 6 of the binding site cavity of the receptors.
