PMID: 11206708Feb 24, 2001Paper

Interaction between the partially insurmountable antagonist valsartan and human recombinant angiotensin II type 1 receptors

Fundamental & Clinical Pharmacology
Ilse VerheijenPatrick Vanderheyden


The interaction between the AT1 receptor-selective antagonist valsartan, and its human receptor, was investigated by direct radioligand binding as well as by its inhibition of angiotensin II induced inositol phosphate accumulation in CHO cells expressing human recombinant AT1 receptors. Specific binding of [3H]-valsartan rapidly reached equilibrium at 37 degrees C. It was saturable and occurred to a homogeneous class of sites with a K(D) of 0.88+/-0.076. It was inhibited by other AT1 receptor antagonists with the same potency order as previously described for the binding of [3H]-angiotensin II and [3H]-candesartan to human AT1 receptors (i.e. candesartan > or = EXP3174 > valsartan = irbesartan = angiotensin II > losartan). When valsartan and angiotensin II were applied simultaneously to the CHO-AT1 cells. the antagonist caused a rightward shift of the angiotensin II concentration response curve. Hence, valsartan interacts with the AT1 receptor in a manner that is competitive with angiotensin II. Pre-incubation of the cells with 0.5, 5 and 50 nM valsartan caused an additional, concentration-dependent, up to 55% decline of the maximal response. The partial nature of this insurmountable inhibition by valsartan was confirmed by bip...Continue Reading


Jun 1, 1992·American Journal of Hypertension·P B TimmermansR D Smith
Apr 19, 1966·Proceedings of the Royal Society of London. Series B, Containing Papers of a Biological Character·H P Rang
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Nov 10, 1995·Regulatory Peptides·M de Gasparo, S Whitebread
Jan 14, 1997·European Journal of Pharmacology·M OjimaK Nishikawa
Jul 8, 1999·European Journal of Pharmacology·F L FierensG Vauquelin

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