Key result
Peptidic ligands induce significant internalization of AT1 receptors, whereas the non-peptidic antagonist DuP753 is far less potent, and receptor activation/G-protein coupling are not required.
Population
Chinese hamster ovary cells expressing rat AngII type 1a or 1b receptors or a mutant of AT1a unable to…
Design
Preclinical
Authors
Loading...
Should not alter AT1 antagonist selection in patients; leaves open ligand-specific trafficking effects in human disease.
Receptor activation and G-protein coupling are not required for AT1a internalization, and peptidic ligands are more potent at inducing internalization than non-peptidic antagonists.
Conchon et al. (1994) studied this question. [Sar1]AngII, [Sar1-Ile8]AngII, and DuP753 was evaluated on Receptor internalization. Peptidic ligands induce significant internalization of AT1 receptors, whereas the non-peptidic antagonist DuP753 is far less potent, and receptor activation/G-protein coupling are not required.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: