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  • Title: Internalization of the rat AT1a and AT1b receptors: pharmacological and functional requirements.
    Author: Conchon S, Monnot C, Teutsch B, Corvol P, Clauser E.
    Journal: FEBS Lett; 1994 Aug 08; 349(3):365-70. PubMed ID: 8050598.
    Abstract:
    The capacity of the angiotensin II (AngII) agonist [Sar1]AngII, the antagonist [Sar1-Ile8]AngII and the non-peptidic antagonist DuP753 to undergo receptor internalization were studied in Chinese hamster ovary cells expressing rat AngII type 1a or 1b receptors (AT1a or AT1b) or a mutant of AT1a (Asn74) unable to couple G-protein. In this expression system, the ligand-induced internalization of rat AT1a and AT1b are similar. Moreover, peptidic ligands, either the agonist or antagonist, induce a significant internalization of AT1 receptors, but the non-peptidic antagonist DuP753 is far less potent. Finally, the normal internalization of the mutant Asn74 demonstrates that receptor activation and G-protein coupling are not required for AT1a internalization.
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