Abstract A new class of α 2-adrenergic receptor antagonists, the 2-(aminobenzyl)-1, 2, 3, 4- tetrahydroisoquinolines 4 and their derivatives, is described. Two synthetic routes are reported. An investigation of the structure-activity relationships including various substitutions of the isoquinoline moiety and the benzyl group is discussed. The affinity and selectivity for both α 1-and α 2-adrenoceptors was defined by studying the displacement of ...