Table 10.
Sequences of AII and AII1–4 and their reported biological properties [115].
| Compound | Sequence | IC50 for AT2R [nM] b | AT2R/AT1R Selectivity c |
|---|---|---|---|
| All a | Asp-Arg-Val-Tyr-Ile-His-Pro-Phe | 0.12 ± 0.01 | 13.7 |
| [Tyr6]All | Asp-Arg-Val-Tyr-Ile-Tyr-Pro-Phe | 4.0 d | 18,000 d |
| All1 | Asp-Arg-Val-Tyr-IleΨ[Tz]Tyr-Pro-Phe | 1990 ± 88 | >5 |
| All2 | Asp-Arg-Val-TyrΨ[Tz]Ile-Tyr-Pro-Phe | 2.8 ± 0.08 | >3611 |
| All3 | Asp-Arg-ValΨ[Tz]Tyr-Ile-Tyr-Pro-Phe | 155 ± 6 | >64 |
| All4 | Asp-ArgΨ[Tz]Val-Tyr-Ile-Tyr-Pro-Phe | 7.5 ± 0.05 | >1336 |
a Reference compound. b Determined in a competition binding assay on HEK-293 cells transfected with AT2R with [125I,Sar1,Ile8]All as competitor. Expressed as means ± SD of three independent experiments. c Ratio of IC50 AT2R/AT1R. d Values taken from Magnani et al. [114].