S. Conchon et al., INTERNALIZATION OF THE RAT AT(1A) AND AT(1B) RECEPTORS - PHARMACOLOGICAL AND FUNCTIONAL REQUIREMENTS, FEBS letters, 349(3), 1994, pp. 365-370
The capacity of the angiotensin II (AngII) agonist [Sar1]AngII, the an
tagonist [Sar1-Ile8]AngII and the non-peptidic antagonist DuP753 to un
dergo receptor internalization were studied in Chinese hamster ovary c
ells expressing rat AngII type 1a or 1b receptors (AT(1a) or AT(1b)) o
r a mutant of AT(1a) (Asn(74)) unable to couple G-protein. In this exp
ression system, the ligand-induced internalization of rat AT(1a) and A
T(1b) are similar. Moreover, peptidic ligands, either the agonist or a
ntagonist, induce a significant internalization of AT(1) receptors, bu
t the non-peptidic antagonist DuP753 is far less potent. Finally, the
normal internalization of the mutant Asn(74) demonstrates that recepto
r activation and G-protein coupling are not required for AT(1a) intern
alization.