Reversible and syntopic interaction between angiotensin receptor antagonists on Chinese hamster ovary cells expressing human angiotensin II type 1 receptors

Biochemical Pharmacology
Patrick VanderheydenG Vauquelin

Abstract

Evidence for a competitive type of interaction between angiotensin II type 1 (AT(1)) antagonists on Chinese hamster ovary cells expressing the human AT(1) receptor (CHO-AT(1)) was obtained by analyzing the binding of [(3)H]-2-ethoxy-1-[(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl]-1H- ben zimidazoline-7-carboxylic acid ([(3)H]candesartan) and by measuring the AT-induced production of inositol phosphates. The AT(1) antagonists candesartan, 2-n-butyl-4-chloro-1-[(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl]+ ++imid azole-5-carboxylic acid (EXP3174), or 2-n-butyl-4-chloro-5-hydroxymethyl-1-[(2'-(1H-tetrazol-5-yl)bip hen yl- 4-yl)methyl]imidazole (losartan) produced a concentration-dependent increase in the apparent K(d) values of [(3)H]candesartan in saturation binding experiments, while the B(max) values were unchanged. Furthermore, the dissociation rate of the radioligand initiated by 1 microM unlabelled candesartan was not changed in the presence of 10 microM losartan, 10 microM EXP3174, or 10 microM irbesartan (2-n-butyl-4-spirocyclopentane-1-[(2'-(1H-tetrazol-5-yl)b iph enyl-4-yl) methyl]2-imidazolin-5-one)). Preincubation of the CHO-AT(1) cells with candesartan, EXP3174, and irbesartan caused a reduction in the maximal AT-induce...Continue Reading

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Citations

Sep 18, 2002·Biochemical Pharmacology·Ilse VerheijenGeorges Vauquelin
Apr 24, 2012·Chemical Reviews·Reem SmoumMorris Srebnik
Jan 22, 2005·Fundamental & Clinical Pharmacology·G Vauquelin, I Van Liefde
Dec 18, 2009·Fundamental & Clinical Pharmacology·Ann PackeuGeorges Vauquelin
Mar 26, 2004·Biochemical Pharmacology·Ilse VerheijenGeorges Vauquelin
Apr 16, 2003·Biochemical Pharmacology·Minh Tam LeGeorges Vauquelin
Jan 19, 2012·Clinical and Experimental Hypertension : CHE·Hiroshi HasegawaIssei Komuro
Jan 30, 2015·Scientific Reports·Samalia DabulAnastasios Lymperopoulos
Mar 29, 2018·Clinical and Experimental Hypertension : CHE·Di ZhaoPingshuan Dong
Mar 23, 2011·Journal of the Renin-angiotensin-aldosterone System : JRAAS· Zhenfeng Zheng Shan Lin
Jul 26, 2002·Journal of Human Hypertension·A H Gradman
Aug 6, 2004·Journal of the Renin-angiotensin-aldosterone System : JRAAS·Trefor MorganRobert Jeffrey MacInnis
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
Jul 21, 2001·Journal of Human Hypertension·D G VidtUNKNOWN CLAIM Study Investigators
Apr 8, 2006·Journal of Hypertension. Supplement : Official Journal of the International Society of Hypertension·Georges VauquelinIsabelle Van Liefde
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
Apr 1, 2005·Journal of Biomolecular Screening·Regine M Van Der HeeEls M De Groene
Jan 26, 2016·British Journal of Pharmacology·Georges VauquelinDavid C Swinney

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