CGP-42112 acetate is a potent angiotensin receptor AT2 agonist that inhibits the increase in protein kinase A activity produced by LPS.

AT2 receptor:0.07-0.3 nM (Kd)

At concentrations of ≥1 nM, CGP-42112 acetate significantly inhibits cGMP production from the basal value and also inhibits TH-enzyme activity from the basal value. The inhibitory effects of CGP-42112 acetate on TH-enzyme activity and cGMP production are nullified by PD123319 (AT(2)-R antagonist), while CV-11974 (AT(1)-R antagonist) is ineffective[1].[125I]CGP-42112 acetate selectively binds to the AT2 angiotensin II receptor subtype. The binding affinity of [125I]CGP-42112 acetate is higher in the brain than in the adrenal. Beta-mercaptoethanol enhances [125I]CGP-42112 acetate binding in the brain but does not alter its binding in the adrenal[2].The high-affinity binding of [125I]CGP-42112 acetate (Kd = 0.07-0.3 nM, depending on the area studied) is selective for AT2 receptors. This selectivity is demonstrated by the lack of competition with the AT1 ligand losartan and competition by the AT2 ligands PD 123177 and unlabeled CGP-42112 acetate, as well as the non-selective peptides Ang II and angiotensin III (Ang III)[3].

Intravenous infusions of CGP-42112 acetate (0.1 and 1 mg kg-1 min-1) and PD 123319 (0.36 and 1 mg kg-1 min-1) shifted the upper limit of CBF autoregulation toward higher blood pressures without affecting baseline CBF[4].