Abstract
Angiotensin II mediates its haemodynamic effects by binding to specific cell-surface receptors. In humans, two receptor subtypes have been identified, designated AT 1 and AT 2 . Because all major 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 -receptor blockers. The relative receptor binding affinities of currently available AT 1 -receptor blockers is candesartan > irbesartan > valsartan/EXP-3174/telmisartan > tasosartan > losartan > eprosartan. Candesartan 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 for 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.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
