Titre du document / Document title
Pharmacology of AT
1-receptor blockers
Auteur(s) / Author(s)
UNGER Thomas
(1) ;
Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)
(1) Christian-Albrechts-University, Kiel, ALLEMAGNE
Résumé / Abstract
Angiotensin II mediates its haemodynamic effects by binding to specific cell-surface receptors. Ii humans, two receptor subtypes have been identified, designated AT
1 and AT
2. Because all majo deleterious effects of angiotensin II are produced via binding to AT
1-receptors, selective blockade of this receptor subtype should confer haemodynamic benefits, while allowing stimulation of the potentially beneficial effects mediated by AT
2-receptors. Experimental studies using various models have consistently revealed marked differences in the receptor binding properties of different AT
1-recepto blockers. The relative receptor binding affinities of currently available AT
1-receptor blockers is candesartan > irbesartan > valsartan/EXP-3174/telmisartan > tasosartan > losartan > eprosartan. Can desartan is also released from the receptor more slowly than other available AT
1-receptor blockers with a half-life of approximately 152 min for the receptor-blocker complex, compared with 31 min fo EXP-3174, 17 min for irbesartan and 5 min for losartan. Candesartan therefore binds to the AT
1-receptor more tightly and more persistently than other AT
1-receptor blockers.
Revue / Journal Title
Blood pressure
ISSN 0803-7051
Source / Source
Congrès
Roundtable Meeting at the 10th European Meeting on Hypertension (EHS), Göteborg
, SUEDE
(31/05/2000)
2001, vol. 10, SUP3 (39 p.) (24 ref.), pp. 5-10
Langue / Language
Anglais
Editeur / Publisher
Taylor & Francis, Stockholm, SUEDE
(1992)
(Revue)
Mots-clés anglais / English Keywords
Hemodynamics ;
Candesartan ;
Irbesartan ;
Valsartan ;
Telmisartan ;
Tasosartan ;
Losartan ;
Eprosartan ;
Angiotensin antagonist ;
Pharmacology ;
Angiotensin II ;
Cell surface ;
Human ;
Chemotherapy ;
Antihypertensive agent ;
Peptides ;
Non peptide compound ;
Mots-clés français / French Keywords
Hémodynamique ;
Candésartan ;
Irbésartan ;
Valsartan ;
Telmisartan ;
Tasosartan ;
Losartan ;
Eprosartan ;
Antagoniste angiotensine ;
Pharmacologie ;
Angiotensine II ;
Surface cellulaire ;
Homme ;
Chimiothérapie ;
Antihypertenseur ;
Peptide ;
Composé non peptide ;
Récepteur angiotensine AT1 ;
Mots-clés espagnols / Spanish Keywords
Hemodinámica ;
Candesartán ;
Irbesartán ;
Valsartán ;
Telmisartán ;
Tasosartán ;
Losartán ;
Eprosartán ;
Antagonista angiotensina ;
Farmacología ;
Angiotensina II ;
Superficie celular ;
Hombre ;
Quimioterapia ;
Antihipertensivo ;
Péptido ;
Compuesto no péptido ;
Localisation / Location
INIST-CNRS, Cote INIST : 26137, 35400009975096.0010
Nº notice refdoc (ud4) : 1117331
