| Bioactivity | CGP-42112 (CGP-42112A) is a potent Angiotensin-II subtype 2 receptor(AT2 R) agonist[1]. | ||||||||||||
| Invitro | CGP-42112 (≥1 nM) significantly inhibits cGMP production from the basal value. CGP-42112 (≥1 nM) significantly inhibits TH-enzyme activity from the basal value. These inhibitory effects of CGP-42112 on TH-enzyme activity and-cGMP production are abolished by PD123319 (AT(2)-R antagonist) while CV-11974 (AT(1)-R antagonist) is ineffective[1]. [125I]CGP-42112 binds selectively to the AT2 angiotensin II receptor subtype. [125I]CGP-42112 binds with higher affinity in the brain than in the adrenal. beta-Mercaptoethanol enhanced [125I]CGP-42112 binding in the brain, but does not alter its binding in the adrenal[2]. [125I]CGP-42112 binds with high affinity (Kd = 0.07-0.3 nM, depending on the area studied). [125I]CGP-42112 binding is selective for AT2 receptors, as determined by lack of competition with the AT1 ligand losartan, and competition by the AT2 ligands PD 123177 and unlabeled CGP-42112 and the non-selective peptides Ang II and angiotensin III (Ang III)[4]. | ||||||||||||
| In Vivo | Intravenous infusions of CGP-42112 (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[3]. | ||||||||||||
| Name | CGP-42112 | ||||||||||||
| CAS | 127060-75-7 | ||||||||||||
| Formula | C52H69N13O11 | ||||||||||||
| Molar Mass | 1052.19 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Takekoshi K, et al. Angiotensin-II subtype 2 receptor agonist (CGP-42112) inhibits catecholamine biosynthesis in cultured porcine adrenal medullary chromaffin cells. Biochem Biophys Res Commun. 2000 Jun 7;272(2):544-50. [2]. Speth RC. [125I]CGP 42112 binding reveals differences between rat brain and adrenal AT2 receptor binding sites. Regul Pept. 1993 Mar 19;44(2):189-97. [3]. Naveri L, et al. Angiotensin II AT2 receptor stimulation extends the upper limit of cerebral blood flow autoregulation: agonist effects of CGP 42112 and PD 123319. J Cereb Blood Flow Metab. 1994 Jan;14(1):38-44. [4]. Heemskerk FM, et al. Quantitative autoradiography of angiotensin II AT2 receptors with [125I]CGP 42112. Brain Res. 1995 Apr 17;677(1):29-38. |