Mechanistic differences of various AT1-receptor blockers in isolated vessels of different origin

Hypertension
P MorsingT Abrahamsson

Abstract

The functional inhibitory characteristics of the angiotensin II type 1 receptor blockers (ARB) candesartan; irbesartan; and losartan and its active metabolite EXP 3174 (EXP) were studied in rabbit aortic strips and rat portal vein preparations in vitro. Moreover, plasma-protein binding was determined, and the binding was high (>98. 5%) for all ARBs. These values were needed to relate the concentrations of the ARBs used in vitro to the nonprotein bound concentrations in clinical use. In both vascular preparations, candesartan caused a marked decrease in the maximal contractile response of the angiotensin II (Ang II) concentration-response curve. Losartan, EXP, and irbesartan caused a rightward parallel shift without any major effects on the maximal response to Ang II. The inhibitory effect of candesartan developed slowly (maximal effect after >30 minutes) and lasted >2 hours despite repeated washing of the vessels. The effect of losartan, irbesartan, and EXP had a faster onset, and most of the inhibitory effect disappeared after washing. The duration of the inhibitory effects of the ARBs were not related to lipophilicity of the compounds. Cooling of the rat portal vein preparations to 4 degrees C before administration of candesa...Continue Reading

References

Oct 1, 1994·Trends in Pharmacological Sciences·M J RobertsonP Leff
Jan 14, 1997·European Journal of Pharmacology·M OjimaK Nishikawa
Mar 31, 1998·Journal of Pharmaceutical Sciences·C von CorswantS Engström
Jul 15, 1998·British Journal of Clinical Pharmacology·C MalerczykE Mutschler
Jan 1, 1955·Quarterly Journal of Experimental Physiology and Cognate Medical Sciences·J H GADDUMF F STEPHENS

❮ Previous
Next ❯

Citations

Feb 10, 2006·Naunyn-Schmiedeberg's Archives of Pharmacology·R Schulz
Feb 15, 2012·Naunyn-Schmiedeberg's Archives of Pharmacology·Georges VauquelinPhilip Seeman
Sep 18, 2002·Biochemical Pharmacology·Ilse VerheijenGeorges Vauquelin
Oct 15, 2010·Hypertension Research : Official Journal of the Japanese Society of Hypertension·Lei LiYunzeng Zou
Mar 10, 2011·Nephrology, Dialysis, Transplantation : Official Publication of the European Dialysis and Transplant Association - European Renal Association·Seung Hyeok HanShin-Wook Kang
Jun 8, 2001·Journal of Cardiovascular Pharmacology·M S BerlowitzT H Le Jemtel
Jan 28, 2003·Journal of Cardiovascular Pharmacology·He-Hui XieDing-Feng Su
Mar 27, 2003·Journal of Cardiovascular Pharmacology·Jun Ming WangFrans H H Leenen
Feb 2, 2000·Current Opinion in Nephrology and Hypertension·R T Gansevoort, D de Zeeuw
Feb 15, 2005·International Journal of Clinical Practice·J-L ImbsUNKNOWN French Collaborative Candesartan Study Group
Jun 8, 2012·High Blood Pressure & Cardiovascular Prevention : the Official Journal of the Italian Society of Hypertension·Claudio Borghi, Arrigo F G Cicero
Nov 28, 2002·European Journal of Heart Failure·Emil PantevMalin Malmsjö
Jul 1, 2006·Future Cardiology·Robert S McKelvie
Nov 19, 2014·Bulletin of Experimental Biology and Medicine·A A SpasovA A Brigadirova
Apr 8, 2006·Journal of Hypertension. Supplement : Official Journal of the International Society of Hypertension·Georges VauquelinIsabelle Van Liefde
Feb 18, 2010·Journal of Hypertension·Franz SchaeferUNKNOWN Candesartan in Children with Hypertension Investigators
Oct 6, 2006·Expert Opinion on Pharmacotherapy·Robert S McKelvie
Jan 3, 2016·Drug Discovery Today. Technologies·Georges VauquelinDavid C Swinney
Dec 19, 2008·The Journal of Clinical Hypertension·Howard TrachtmanUNKNOWN Candesartan in Children with Hypertension (CINCH) Investigators
Mar 27, 2007·Pharmacotherapy·Mark E Dunlap
Jul 9, 2010·Fundamental & Clinical Pharmacology·Marie WennerbergGeorges Vauquelin
Oct 1, 2010·British Journal of Pharmacology·Georges Vauquelin, Steven J Charlton
Jan 5, 2005·Peptides·Ecio Alves NascimentoDurval Rosa Borges
Feb 14, 2003·Journal of the Renin-angiotensin-aldosterone System : JRAAS·Nish ChaturvediUNKNOWN DIRECT Programme Study Group
Nov 26, 2011·The Annals of Pharmacotherapy·William L Baker, William B White
May 19, 2004·American Journal of Physiology. Heart and Circulatory Physiology·Ikuyo KusakaJiping Tang
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

❮ Previous
Next ❯

Related Concepts

Related Feeds

Antihypertensive Agents: Mechanisms of Action

Antihypertensive drugs are used to treat hypertension (high blood pressure) which aims to prevent the complications of high blood pressure, such as stroke and myocardial infarction. Discover the latest research on antihypertensive drugs and their mechanism of action here.

Anthelmintics

Anthelmintics or antihelminthics are a group of antiparasitic drugs that expel parasitic worms (helminths) and other internal parasites from the body by either stunning or killing them and without causing significant damage to the host. Discover the latest research on anthelmintics here.