Long-lasting angiotensin type 1 receptor binding and protection by candesartan: comparison with other biphenyl-tetrazole sartans

Journal of Hypertension. Supplement : Official Journal of the International Society of Hypertension
Georges VauquelinIsabelle Van Liefde

Abstract

The ability of biphenyl-tetrazole angiotensin type 1 (AT1) receptor antagonists (BTsartans) to block angiotensin II (Ang II)-mediated responses has been extensively investigated in vascular tissues and, more recently, in cell lines expressing the human AT1-receptor. When pre-incubated, BTsartans acted surmountably (shifting the Ang II concentration-response curve to the right) or insurmountably (also decreasing the maximal response). It was shown that their insurmountable behaviour is due to the formation of tight, long-lasting complexes with the receptor. Partial insurmountable antagonism is due to the co-existence of tight and loose complexes. The proportion of insurmountable antagonism, the potency and the dissociation rate of the BTsartans decreases in the order: candesartan > EXP3174 (losartan's active metabolite) > valsartan > irbesartan > losartan. It is of interest to explore how tight AT1-receptor binding of BTsartans such as candesartan might contribute to their long-lasting clinical effect. Computer-assisted simulations (COPASI program) were performed to follow the receptor-occupation and protection by different antagonists as a function of time. Free antagonist concentrations were allowed to decrease exponentially w...Continue Reading

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Citations

Feb 15, 2012·Naunyn-Schmiedeberg's Archives of Pharmacology·Georges VauquelinPhilip Seeman
Apr 2, 2011·Future Cardiology·Kevin E C Meyers, Brittany Behar
Mar 23, 2011·Expert Opinion on Drug Metabolism & Toxicology·Michel Burnier, Grégoire Wuerzner
Jan 19, 2012·Clinical and Experimental Hypertension : CHE·Hiroshi HasegawaIssei Komuro
Mar 7, 2007·Diabetes Research and Clinical Practice·José A García Donaire, Luis M Ruilope
Feb 11, 2012·International Journal of Urology : Official Journal of the Japanese Urological Association·Ken AikawaOsamu Yamaguchi
Jan 11, 2013·International Journal of Hypertension·Hanna Andersson, Mathias Hallberg
Nov 19, 2013·International Journal of Cardiology·Hae Chang JeongUNKNOWN Korea Acute Myocardial Infarction Registry Investigators
Mar 29, 2018·Clinical and Experimental Hypertension : CHE·Di ZhaoPingshuan Dong
Jun 28, 2011·Nature Reviews. Drug Discovery·David C Swinney, Jason Anthony
Dec 13, 2019·Biochimica Et Biophysica Acta. Biomembranes·Sofia KiriakidiThomas Mavromoustakos
Apr 3, 2021·Nuclear Medicine and Biology·Aida M Abreu DiazJean N DaSilva
Feb 5, 2021·Journal of Virology·Nichole Orr-BurksRalph A Tripp
Apr 17, 2008·Biochemistry·Peter J Tummino, Robert A Copeland

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