The synthesis of a series of 4-(6, 7-dimethoxy-1, 2, 3, 4-tetrahydroisoquinolin-2-yl) methyl-2- arylbenzofuran and 4-(6, 7-dimethoxy-1, 2, 3, 4-tetrahydroisoquinolin-2-yl) methylbenzofuran-2-carboxamide derivatives as novel α2C-adrenergic receptor antagonists are described. Their affinity at three different human α2-adrenergic receptors is reported, and some of these compounds exhibited high affinity for the α2C-adrenergic receptor with ...