How can the differences among AT1-receptor antagonists be explained?

Cell Biochemistry and Biophysics
P Morsing, G Vauquelin

Abstract

Over the last few years we have seen a new class of antihypertensive drug evolve, the angiotensin II subtype 1 receptor antagonists. Hypothetically, all substances in this class should have the same effect on blood pressure and on end-organ damage as they all block the AT1 receptor. However, there are distinctions between them that may explain the significant and clinically important differences that seem to exist within this class of drug. An explanation for the differences may be found in receptor-antagonist kinetics. The receptor-antagonist interaction may be fitted to a two-state, two-step model which determines how large a part of the binding that will be surmountable and how large a part that will be insurmountable. The proportion of surmountable/insurmountable binding fits nicely to the duration of binding of the antagonist to the receptor, which may be translated into efficacy for the antagonist as outlined in the following review.

Citations

Jun 23, 2005·Current Medical Research and Opinion·Gerd Bönner, Winfried Fuchs
Apr 29, 2005·International Journal of Clinical Practice·L R Erhardt
Mar 4, 2011·The Journal of Clinical Hypertension·David RussellSverre E Kjeldsen
Feb 20, 2014·Medicinal Research Reviews·Dong GuoLaura H Heitman
Apr 28, 2011·The Journal of Physical Chemistry. B·Charalambos FotakisMaria Zervou
Oct 13, 2005·Journal of Cardiovascular Pharmacology·David E MireMichael K Pugsley
Jul 26, 2002·Journal of Human Hypertension·A H Gradman

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