A series of 4-amino-2-[4-(1, 4-benzodioxan-2-ylcarbonyl) piperazin-l-yl]-6, 7- dimethoxyquinazoline derivatives was synthesized for evaluation as a-antagonists and antihypertensive agents. Most compounds displayed high (nM) binding affinity for a,- adrenoceptors with no significant activity at a2-sites. Selective antagonism of the a,- mediated vasoconstrictor effects of norepinephrine is also characteristic of the series. ...