title: Internalization of the rat AT1a and AT1b receptors: pharmacological and functional requirements.
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.
authors.affiliation: Institut National de la Santé et de la Recherche Médicale Unité 36 Collège de France, Paris.
authors.forename: S
authors.initials: S
authors.lastname: Conchon
authors.forename: C
authors.initials: C
authors.lastname: Monnot
authors.forename: B
authors.initials: B
authors.lastname: Teutsch
authors.forename: P
authors.initials: P
authors.lastname: Corvol
authors.forename: E
authors.initials: E
authors.lastname: Clauser
mesh_terms: D000804:Angiotensin II / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors* / Q000378:metabolism; D057911:Angiotensin Receptor Antagonists; D000818:Animals; D001692:Biological Transport; D001713:Biphenyl Compounds / Q000378:metabolism*; D016466:CHO Cells; D006224:Cricetinae; D004305:Dose-Response Relationship, Drug; D007093:Imidazoles / Q000378:metabolism*; D019808:Losartan; D051381:Rats; D011945:Receptors, Angiotensin / Q000145:classification / Q000235:genetics / Q000378:metabolism*; D011994:Recombinant Proteins / Q000378:metabolism; D013777:Tetrazoles / Q000378:metabolism*
chemical_list: D057911:Angiotensin Receptor Antagonists; D001713:Biphenyl Compounds; D007093:Imidazoles; D011945:Receptors, Angiotensin; D011994:Recombinant Proteins; D013777:Tetrazoles; D000804:Angiotensin II; C009210:sarleucin; C074793:angiotensin II, Sar(1)-; D019808:Losartan