Angiotensin II Receptor Ligand

Names

[ Name ]:
Angiotensin II Receptor Ligand

[Synonym ]:
L-Isoleucine, N-[N-(diaminomethylene)-N-[(phenylmethoxy)carbonyl]-L-ornithyl]-N-[N-(3-pyridinylcarbonyl)-L-tyrosyl]-L-lysyl-L-histidyl-L-prolyl-
MFCD00133611
N-{N-[(Benzyloxy)carbonyl]-N-(diaminomethylene)-L-ornithyl}-N-[N-(3-pyridinylcarbonyl)-L-tyrosyl]-L-lysyl-L-histidyl-L-prolyl-L-isoleucine
CGP-42112

Biological Activity

[Description]:

CGP-42112(CGP-42112A) is a potent Angiotensin-II subtype 2 receptor(AT2 R) agonist.IC50 value:Target: AT2 R agonistin vitro: CGP42112 (>==1 nM) significantly inhibited cGMP production from the basal value. CGP42112 (>==1 nM) significantly inhibited TH-enzyme activity from the basal value. These inhibitory effects of CGP42112 on TH-enzyme activity and-cGMP production were abolished by PD123319 (AT(2)-R antagonist) while CV-11974 (AT(1)-R antagonist) was ineffective [1]. [125I]CGP 42112 bound selectively to the AT2 angiotensin II receptor subtype. [125I]CGP 42112 bound with higher affinity in the brain than in the adrenal. beta-Mercaptoethanol enhanced [125I]CGP 42112 binding in the brain, but did not alter its binding in the adrenal [2]. [125I]CGP 42112 bound with high affinity (Kd = 0.07-0.3 nM, depending on the area studied). [125I]CGP 42112 binding was 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].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Angiotensin Receptor

Research Areas >> Neurological Disease

[References]

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C₅₂H₆₉N₁₃O₁₁

[ Molecular Weight ]:
1052.185

[ Exact Mass ]:
1051.523926

[ PSA ]:
365.14000

[ LogP ]:
2.38

[ Index of Refraction ]:
1.659

[ Storage condition ]:
2-8℃

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Safety Phrases ]:
S22-S24/25

[ RIDADR ]:
NONH for all modes of transport

Articles

Altered efficacy of AT1R-targeted treatment after spontaneous cancer cell-AT1R upregulation.

BMC Cancer 11 , 274, (2011)

Targeting of the renin angiotensin system (RAS) reduces tumour growth in experimental models of cancer. We aimed to establish if combined targeting of the 'classical' and 'alternative' arms of the RAS...

Update on the angiotensin AT(2) receptor.

Curr. Hypertens. Rep. 15(1) , 25-30, (2013)

It is quite well established that activation of the AT(2) receptor (AT(2)R) provides a counter-regulatory role to AT(1)R overactivity, particularly during pathological conditions. Indeed, a potential ...

Angiotensin III modulates the nociceptive control mediated by the periaqueductal gray matter

Neuroscience 164(3) , 1263-73, (2009)

Endogenous angiotensin (Ang) II and/or an Ang II-derived peptide, acting on Ang type 1 (AT1) and Ang type 2 (AT2) receptors, can carry out part of the nociceptive control modulated by periaqueductal g...