Binding of the antagonist [3H]candesartan to angiotensin II AT1 receptor-transfected [correction of tranfected] Chinese hamster ovary cells

European Journal of Pharmacology
F L FierensG Vauquelin

Abstract

Binding of the non-peptide angiotensin II AT1 antagonist [3H](2-ethoxy-1-[(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl]- H-benzimidazoline-7-carboxylic acid ([3H]candesartan) to human angiotensin II AT1 receptor-transfected Chinese hamster ovary (CHO-AT1) cells was inhibited to the same extent by angiotensin II and non-peptide angiotensin II AT1 antagonists. No binding was observed in control CHO-K1 cells. Dissociation was slow (k(-1) = 0.0010+/-0.0001 min(-1)) after removal of the free [3H]candesartan but increased 5-fold upon addition of supramaximal concentrations of angiotensin II AT1 antagonists. Angiotensin II responses recovered equally slow from candesartan-pretreatment. When washed and further incubated, these angiotensin II responses also recovered more rapidly in the presence of 2-n-butyl-4-chloro-5-hydroxymethyl-1-[(2'-(1H-tetrazol-5-yl)biphen yl-4-yl)methyl]imidazole (losartan), indicating that unlabelled ligands prevented reassociation. [3 H]candesartan saturation binding experiments required a long time to reach equilibrium. Therefore, the equilibrium dissociation constant (Kd = 51+/-8 pM) was calculated from the association and dissociation rate constants. Our findings indicate that the insurmountable nature of ca...Continue Reading

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Citations

Aug 28, 2010·Naunyn-Schmiedeberg's Archives of Pharmacology·Peter HeuslerDidier Cussac
Apr 27, 2001·Biochemical Pharmacology·F L FierensaG Vauquelin
Sep 18, 2002·Biochemical Pharmacology·Ilse VerheijenGeorges Vauquelin
Dec 31, 2002·European Journal of Pharmacology·Catherina Caballero-GeorgeArnold Vlietinck
Jul 8, 1999·European Journal of Pharmacology·F L FierensG Vauquelin
Mar 4, 2000·Lancet·M Burnier, H R Brunner
Mar 14, 2002·Regulatory Peptides·Minh Tam LeGeorges Vauquelin
Sep 2, 2004·Nature Reviews. Drug Discovery·David C Swinney
Feb 7, 2003·Fundamental & Clinical Pharmacology·G VauquelinP M L Vanderheyden
Jul 1, 2006·Future Cardiology·Robert S McKelvie
Jan 19, 2012·Clinical and Experimental Hypertension : CHE·Hiroshi HasegawaIssei Komuro
Oct 6, 2006·Expert Opinion on Pharmacotherapy·Robert S McKelvie
Mar 29, 2018·Clinical and Experimental Hypertension : CHE·Di ZhaoPingshuan Dong
Aug 25, 2017·British Journal of Pharmacology·Georges Vauquelin
Jul 26, 2002·Journal of Human Hypertension·A H Gradman
Feb 3, 2004·The Journal of Biological Chemistry·Takanobu TakezakoSadashiva S Karnik
Feb 15, 2001·Circulation·M Burnier
Mar 1, 2001·Journal of the Renin-angiotensin-aldosterone System : JRAAS·Georges VauquelinPatrick Ml Vanderheyden
Mar 1, 2001·Journal of the Renin-angiotensin-aldosterone System : JRAAS·Georges VauquelinPatrick Ml Vanderheyden
Apr 23, 2002·Journal of the Renin-angiotensin-aldosterone System : JRAAS·P M VanderheydenG Vauquelin
Aug 26, 2009·Fundamental & Clinical Pharmacology·M WennerbergGeorges Vauquelin
Oct 1, 2010·British Journal of Pharmacology·Georges Vauquelin, Steven J Charlton
Apr 8, 2006·Journal of Hypertension. Supplement : Official Journal of the International Society of Hypertension·Georges VauquelinIsabelle Van Liefde
May 3, 2016·British Journal of Clinical Pharmacology·Georges Vauquelin
Nov 24, 2006·American Journal of Physiology. Cell Physiology·Julia L CookRichard N Re
Jun 19, 2007·The Journal of Pharmacology and Experimental Therapeutics·Erik LindströmGeorges Vauquelin
Aug 17, 2002·The Journal of Pharmacology and Experimental Therapeutics·Marc P MaillardMichel Burnier
Jan 18, 2013·Journal of Hypertension·Maarten A D H Schalekamp, A H Jan Danser
Nov 6, 2012·Cardiovascular Therapeutics·Joel M Neutel, David H G Smith
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Oct 31, 2001·Blood Pressure. Supplement·T Unger
Jul 9, 2010·Fundamental & Clinical Pharmacology·Marie WennerbergGeorges Vauquelin

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