AT1R antagonist 3 (Compound 1) is an antagonist for angiotensin II type 1 receptor ( AT1R ) and an inhibitor for calcium channel type-L CaV 1.2 ( IC 50 =0.57 μM). AT1R antagonist 3 exhibits vasodilation efficacy in solated rat aorta (10 μM, 88.7%) and antihypertensive efficacy in rat models.