Distinction between surmountable and insurmountable selective AT1 receptor antagonists by use of CHO-K1 cells expressing human angiotensin II AT1 receptors

British Journal of Pharmacology
Patrick VanderheydenGeorges Vauquelin

Abstract

1. CHO-K1 cells that were stably transfected with the gene for the human AT1 receptor (CHO-AT1 cells) were used for pharmacological studies of non-peptide AT1 receptor antagonists. 2. In the presence of 10 mM LiCl, angiotensin II caused a concentration-dependent and long-lasting increase of inositol phosphates accumulation with an EC50 of 3.4 nM. No angiotensin II responses are seen in wild-type CHO-K1 cells. 3. [3H]-Angiotensin II bound to cell surface AT1 receptors (dissociates under mild acidic conditions) and is subject to rapid internalization. 4. Non-peptide selective AT1 antagonists inhibited the angiotensin II (0.1 microM) induced IP accumulation and the binding of [3H]-angiotensin II (1 nM) with the potency order: candesartan > EXP3174 > irbesartan > losartan. Their potencies are lower in the presence of bovine serum albumin. 5. Preincubation with the insurmountable antagonist candesartan decreased the maximal angiotensin II induced inositol phosphate accumulation up to 94% and, concomitantly, decreased the maximal binding capacity of the cell surface receptors. These inhibitory effects were half-maximal for 0.6 nM candesartan and were attenuated by simultaneous preincubation with 1 microM losartan indicating a syntopi...Continue Reading

References

Dec 1, 1992·American Journal of Hypertension·P B TimmermansR D Smith
Dec 1, 1992·Journal of Hypertension. Supplement : Official Journal of the International Society of Hypertension·M A SchalekampA H van den Meiracker
Jun 1, 1992·American Journal of Hypertension·P B TimmermansR D Smith
Feb 28, 1992·Biochemical and Biophysical Research Communications·H FurutaT Inagami
Feb 1, 1991·Trends in Pharmacological Sciences·P B TimmermansW F Herblin
Jul 7, 1983·Journal of Theoretical Biology·A Gero
Jan 1, 1995·Journal of Cardiovascular Pharmacology·S MochizukiA Tomiyama
Mar 1, 1995·Journal of Cardiovascular Pharmacology·A R RenzettiA Giachetti
Oct 1, 1994·Trends in Pharmacological Sciences·M J RobertsonP Leff
Jan 27, 1995·The Journal of Biological Chemistry·S PerlmanT W Schwartz
Jan 14, 1997·European Journal of Pharmacology·M OjimaK Nishikawa
Mar 1, 1959·British Journal of Pharmacology and Chemotherapy·O ARUNLAKSHANA, H O SCHILD
Jan 1, 1955·Quarterly Journal of Experimental Physiology and Cognate Medical Sciences·J H GADDUMF F STEPHENS

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Citations

Aug 14, 2001·Pharmazie in unserer Zeit·R Hübner, W Fuchs
Sep 18, 2009·Analytical and Bioanalytical Chemistry·Matthias GriessnerFrank F Bier
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 14, 2002·Regulatory Peptides·Minh Tam LeGeorges Vauquelin
Sep 6, 2003·Journal of the American College of Cardiology·Kwang Kon KohEak Kyun Shin
Oct 29, 2000·British Journal of Pharmacology·J F LarrivéeF Marceau
Jan 5, 2001·British Journal of Pharmacology·D H WrightK M Metters
Aug 24, 2013·The Journal of Biological Chemistry·Christian BergmayrChristian W Gruber
Aug 5, 2005·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Pandi Vijayapandi, Anantha Naik Nagappa
Dec 31, 2010·Vascular Health and Risk Management·Maria Leonarda De Rosa
Nov 28, 2002·European Journal of Heart Failure·Emil PantevMalin Malmsjö
Sep 1, 2011·Expert Review of Cardiovascular Therapy·Zeeshan Khawaja, Christopher S Wilcox
Feb 18, 2014·Journal of the Renin-angiotensin-aldosterone System : JRAAS·Alexandros NikolaouJo A Van Ginderachter
Jan 30, 2015·Scientific Reports·Samalia DabulAnastasios Lymperopoulos
Jun 27, 2017·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Takanobu TakezakoKoichi Node
May 19, 2004·American Journal of Physiology. Heart and Circulatory Physiology·Ikuyo KusakaJiping Tang
Jul 26, 2002·Journal of Human Hypertension·A H Gradman
May 4, 2011·Journal of Peptide Science : an Official Publication of the European Peptide Society·Aneta LukaszukDirk Tourwé
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·Hoa Ytterberg, Lars Edvinsson
Mar 1, 2001·Journal of the Renin-angiotensin-aldosterone System : JRAAS·William F van RodijnenPiet M Ter Wee
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·N K Hollenberg, P S Sever
Apr 23, 2002·Journal of the Renin-angiotensin-aldosterone System : JRAAS·P M VanderheydenG Vauquelin

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