Insurmountable non-peptide AT1 receptor antagonism: revealing the molecular mechanisms.

Frederik Fierens

Onderzoeksoutput: PhD Thesis

Samenvatting

The ability of biphenyltetrazole AT1 receptor antagonists (BTsartans) to block angiotensin II (Ang II)- mediated responses has been extensively investigated in vascular tissues and, more recently, in cell lines expressing the human AT1 receptor. When pre-incubated, BTsartans acted surmountably (shifting the Ang II concentration-response curve to the right) or insurmountably (also decreasing the maximal response). It was shown that their insurmountable behaviour is due to the formation of tight, long lasting complexes with the receptor. Partial insurmountable antagonism is due to the co-existence of tight- and loose complexes. The proportion of insurmountable antagonism, the potency and the dissociation rate of the BTsartans decreases in the order: candesartan > EXP3174 (losartans active metabolite) > valsartan > irbesartan >> losartan.
Originele taal-2English
Toekennende instantie
  • Vrije Universiteit Brussel
Begeleider(s)/adviseur
  • Vauquelin, Georges, Promotor
Plaats van publicatieBrussels
StatusPublished - 2002

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