TABLE 2

Activation of Gq, βarrestin1, βarrestin2, and G12 by AT1 receptor ligands

HEK293 cells expressing the AT1 receptor were assayed as described in Materials and Methods. EC50 and Emax are expressed as the means ± S.D. of values obtained in at least three independent experiments performed in triplicate.

GqβArrestin1βArrestin2G12
EC50EmaxEC50EmaxEC50EmaxEC50Emax
nM% AngIInM% AngIInM% AngIInM% AngII
AngII2.4 ± 1.61006.1 ± 1.71004.6 ± 1.91004.7 ± 1.9100
[Sar1]AngII3.3 ± 0.898 ± 86.4 ± 3.0100 ± 15.6 ± 2.394 ± 55.1 ± 2.0104 ± 8
[Ile4]AngII3104 ± 10667 ± 22802 ± 67072 ± 63829 ± 64984 ± 81056 ± 32160 ± 9
[Sar1Ile4]AngII686 ± 5243 ± 7429 ± 12681 ± 4458 ± 15886 ± 3228 ± 6265 ± 5
[Ile8]AngIINRNR7.0 ± 1.654 ± 65.7 ± 2.759 ± 63.5 ± 1.442 ± 5
[Sar1Ile8]AngIINRNR4.5 ± 1.956 ± 65.6 ± 2.061 ± 81.0 ± 0.644 ± 6
AngIII51 ± 1987 ± 854 ± 894 ± 348 ± 1693 ± 990 ± 3398 ± 7
[Ile8]AngIIINRNR11.3 ± 1.050 ± 1049 ± 248 ± 1112.3 ± 7.138 ± 6
  • NR, no response.