Why the study?
Does the degree of selectivity for AT1 over AT2 receptors affect the clinical performance of angiotensin receptor blockers?
Does the degree of selectivity for AT1 over AT2 receptors affect the clinical performance of angiotensin receptor blockers?
This review highlights that ARBs are not a homogenous class and that differences in AT1/AT2 receptor selectivity may translate into distinct organ-protective benefits.
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ARBs may not be interchangeable; leaves open whether AT1 selectivity drives differential outcomes in trials.
During the last decade, angiotensin-receptor blockers have established themselves as effective antihypertensive agents with impressive safety profile and placebo-like tolerability. Additionally, these compounds provide benefits beyond the reduction in blood pressure, in conditions such as heart failure and in patients with type 2 diabetes and renal insufficiency. It is tempting to group all angiotensin-receptor blockers together as a class, but a closer look reveals differences, for example, in chemical structure, metabolism, dissociation rates, and receptor affinities. Recent findings on the respective roles of the angiotensin receptors AT(1) and AT(2) have raised the possibility that the degree of selectivity for AT(1) over AT(2) might affect the performance of the drug. This review attempts to put the concept of selectivity in context and to assess the potential benefits in different organs, with focus on the kidney, endothelium and the heart.
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Helmy M. Siragy (2002) studied this question.
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