Telmisartan has the strongest binding affinity to angiotensin II type 1 receptor: comparison with other angiotensin II type 1 receptor blockers.

摘要: There is a growing body of evidence that the renin-angiotensin system (RAS) plays pivotal role in pathogenesis cardiovascular diseases. Indeed, large clinical trials have demonstrated substantial benefit blockade this for cardiovascular-organ protection. Although several types angiotensin II type 1 (AT1) receptor blockers (ARBs) are commercially available treatment patients with hypertension, comparisons binding affinity to AT1 among them remain be elucidated. In study, we examined dissociation rate ARBs from vitro. Angiotensin time-dependently dissociated telmisartan, olmesartan, candesartan, valsartan, losartan and an active metabolite losartan, EXP3174, membrane components containing human The constant each ARB was 0.003248, 0.004171, 0.005203, 0.009946, 0.01027 0.008561 min(-1), corresponding half-lives 213, 166, 133, 70, 67 81 min, respectively. These results demonstrate telmisartan has strongest various herein. rank order > olmesartan candesartan EXP3174 or = valsartan losartan. present findings suggest (Micardis) may long-lasting blood pressure-lowering effects superior cardioprotective properties hypertension due its antagonistic ability.