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Chemical Compound Review

C160_SIGMA     (2S,3S)-2-[[(2S)-1-[(2S)-2- [[(2S)-6-[[(2S)...

Synonyms: Cgp-42112A, AC1L3XAY, CGP42112A, Cgp 42112, LS-183538, ...
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High impact information on CGP42112A

  • CGP 42112B did not modify the renal blood flow, but dose-dependently decreased urine flow and natriuresis [1].
  • Ang II-induced DNA synthesis (assessed by [3H]thymidine uptake) was significantly increased by PD123319, and the AT2-R agonist CGP42112A reduced the serum-stimulated increase in cell numbers by 23% [2].
  • Only Ang-II type 1 (AT1) receptor-specific antagonists were potent inhibitors of hormone-evoked [3H]inositol phosphate accumulation (DuP 753 IC50 approximately 7 nM compared to CGP 42112A IC50 > 1 microM) [3].
  • Interestingly, competition binding experiments, using 125I-[Sar1]AII as a tracer ligand, showed that the Y292F receptor displayed an increased Ki value for DuP 753, an AT1-specific nonpeptide antagonist and a greatly decreased Ki value for the AT2-specific ligand CGP 42112A [4].
  • Receptor binding assays were performed using a nonselective ligand, [Sar1,Ile8]angiotensin II, or AT2-selective CGP42112A [5].

Biological context of CGP42112A


Anatomical context of CGP42112A

  • In nonpregnant myometrium (n = 5), receptor density [maximum binding capacity (Bmax)] and dissociation constant (Kd) for AT2-selective CGP42112A were 287 +/- 46 fmol/mg protein and 0.48 +/- 0.09 nM, respectively [10].
  • The partial agonist of AT(2) receptors, CGP-42112A, exerted effects on Ang II responses, whereas the AT(1) antagonist ZD7155 did not, suggesting that Ang II responses in CC astrocytes are predominantly mediated by activation of AT(2) receptors [11].
  • The AT2 selective peptide antagonist, CGP 42112A, had a low affinity in AII three membranes (IC50 = 450-1050 nM), whereas the nonpeptide AT2 selective antagonist, WL-19, had no activity at concentrations up to 10 microM [12].
  • AngIV displaces [125I]-AngIV bound to cultured rabbit cardiac fibroblasts whereas AngII receptor-specific ligands ([Sar1, Ile8]-AngII, Dup753, CGP42112A) do not [13].
  • Binding characteristics of CGP42112A (Kd = 0.18 nM, Bmax = 10.8 pmol/mg protein) and ligand specificity were indistinguishable from those obtained with the whole rat fetus and with transiently transfected COS-7 cells [14].

Associations of CGP42112A with other chemical compounds

  • Comparison of binding affinities at AT1B receptor sites with antagonist potencies in the adenylyl cyclase assay show good agreement for losartan and CGP 42112A, whereas PD 123319 is less potent than expected from membrane binding assays, possibly because of partial agonist properties.(ABSTRACT TRUNCATED AT 250 WORDS)[15]
  • In contrast, either the angiotensin subtype 1 (AT1) antagonist DuP 753 or the subtype 2 (AT2) antagonist CGP42112A significantly attenuated the prostaglandin release in response to angiotensin I [16].
  • Angiotensin II elicited time (30 min-24 h)- and concentration (10 nM-1 microM)-dependent increases in PP2A activity in these cells, an effect mimicked by the AT2 receptor ligand CGP-42112A [17].
  • PEt production by 100 nM Ang II was significantly attenuated by the AT1 antagonists losartan, its metabolite EXP 3174 or L-158,809 (all at 1 microM), whereas a similar concentration of the AT2 antagonists CGP 42112A or PD 123177 was ineffective [18].
  • Although the effects of AII and AIII in C1 and parent NG108-15 cells were totally inhibited by the AT1 receptor-selective nonpeptide antagonist, DUP-753 (0.3-1 microM), the AT2-selective antagonists, EXP-655 and CGP42112A (1-10 microM), failed to block the effects of AII [19].

Gene context of CGP42112A


Analytical, diagnostic and therapeutic context of CGP42112A


  1. Subtype 2 of angiotensin II receptors controls pressure-natriuresis in rats. Lo, M., Liu, K.L., Lantelme, P., Sassard, J. J. Clin. Invest. (1995) [Pubmed]
  2. Angiotensin type 2 receptors are reexpressed by cardiac fibroblasts from failing myopathic hamster hearts and inhibit cell growth and fibrillar collagen metabolism. Ohkubo, N., Matsubara, H., Nozawa, Y., Mori, Y., Murasawa, S., Kijima, K., Maruyama, K., Masaki, H., Tsutumi, Y., Shibazaki, Y., Iwasaka, T., Inada, M. Circulation (1997) [Pubmed]
  3. Angiotensin II stimulates the release of phospholipid-derived second messengers through multiple receptor subtypes in heart cells. Lokuta, A.J., Cooper, C., Gaa, S.T., Wang, H.E., Rogers, T.B. J. Biol. Chem. (1994) [Pubmed]
  4. Tyr292 in the seventh transmembrane domain of the AT1A angiotensin II receptor is essential for its coupling to phospholipase C. Marie, J., Maigret, B., Joseph, M.P., Larguier, R., Nouet, S., Lombard, C., Bonnafous, J.C. J. Biol. Chem. (1994) [Pubmed]
  5. Growth-dependent induction of angiotensin II type 2 receptor in rat mesangial cells. Goto, M., Mukoyama, M., Suga, S., Matsumoto, T., Nakagawa, M., Ishibashi, R., Kasahara, M., Sugawara, A., Tanaka, I., Nakao, K. Hypertension (1997) [Pubmed]
  6. Changes in the baroreflex control of heart rate produced by central infusion of selective angiotensin antagonists in hypertensive rats. Oliveira, D.R., Santos, R.A., Santos, G.F., Khosla, M., Campagnole-Santos, M.J. Hypertension (1996) [Pubmed]
  7. Angiotensin II receptor subtypes and biological responses in the adrenal cortex and medulla. Balla, T., Baukal, A.J., Eng, S., Catt, K.J. Mol. Pharmacol. (1991) [Pubmed]
  8. Interaction of angiotensin II with the angiotensin type 2 receptor inhibits the cardiac transient outward potassium current. Caballero, R., Gómez, R., Moreno, I., Nuñez, L., González, T., Arias, C., Guizy, M., Valenzuela, C., Tamargo, J., Delpón, E. Cardiovasc. Res. (2004) [Pubmed]
  9. Prostaglandins contribute to impaired angiotensin II-induced cerebral vasodilation after brain injury. Baranov, D., Armstead, W.M. J. Neurotrauma (2002) [Pubmed]
  10. Type 2 angiotensin II receptor is expressed in human myometrium and uterine leiomyoma and is down-regulated during pregnancy. Matsumoto, T., Sagawa, N., Mukoyama, M., Tanaka, I., Itoh, H., Goto, M., Itoh, H., Horiuchi, M., Dzau, V.J., Mori, T., Nakao, K. J. Clin. Endocrinol. Metab. (1996) [Pubmed]
  11. Membrane currents elicited by angiotensin II in astrocytes from the rat corpus callosum. Montiel-Herrera, M., Miledi, R., García-Colunga, J. Glia (2006) [Pubmed]
  12. Characterization of renal angiotensin II receptors using subtype selective antagonists. Edwards, R.M., Stack, E.J., Weidley, E.F., Aiyar, N., Keenan, R.M., Hill, D.T., Weinstock, J. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  13. A specific binding site for angiotensin II(3-8), angiotensin IV, in rabbit cardiac fibroblasts. Wang, L., Eberhard, M., Kohler, E., Erne, P. J. Recept. Signal Transduct. Res. (1995) [Pubmed]
  14. Characterization of a rat type 2 angiotensin II receptor stably expressed in 293 cells. Mukoyama, M., Horiuchi, M., Nakajima, M., Pratt, R.E., Dzau, V.J. Mol. Cell. Endocrinol. (1995) [Pubmed]
  15. A novel angiotensin receptor subtype in rat mesangium. Coupling to adenylyl cyclase. Zhou, J., Ernsberger, P., Douglas, J.G. Hypertension (1993) [Pubmed]
  16. Stimulation of endothelial cell prostaglandin production by angiotensin peptides. Characterization of receptors. Jaiswal, N., Diz, D.I., Chappell, M.C., Khosla, M.C., Ferrario, C.M. Hypertension (1992) [Pubmed]
  17. Angiotensin II type 2 receptor-mediated stimulation of protein phosphatase 2A in rat hypothalamic/brainstem neuronal cocultures. Huang, X.C., Richards, E.M., Sumners, C. J. Neurochem. (1995) [Pubmed]
  18. Vascular smooth-muscle cells contain AT1 angiotensin receptors coupled to phospholipase D activation. Freeman, E.J., Tallant, E.A. Biochem. J. (1994) [Pubmed]
  19. AT1 angiotensin receptors mobilize intracellular calcium in a subclone of NG108-15 neuroblastoma cells. Ransom, J.T., Sharif, N.A., Dunne, J.F., Momiyama, M., Melching, G. J. Neurochem. (1992) [Pubmed]
  20. Charge heterogeneity of the AT1 angiotensin II receptor subtype in the rat lung. Montiel, M., Quesada, J., Jiménez, E. J. Endocrinol. (1995) [Pubmed]
  21. Angiotensin II type 2 receptor inhibits vascular endothelial growth factor-induced migration and in vitro tube formation of human endothelial cells. Benndorf, R., Böger, R.H., Ergün, S., Steenpass, A., Wieland, T. Circ. Res. (2003) [Pubmed]
  22. Angiotensin-induced cyclic GMP production is mediated by multiple receptor subtypes and nitric oxide in N1E-115 neuroblastoma cells. Zarahn, E.D., Ye, X., Ades, A.M., Reagan, L.P., Fluharty, S.J. J. Neurochem. (1992) [Pubmed]
  23. Receptor subtype that mediates the neuronal effects of angiotensin II in the rat dorsal medulla. Barnes, K.L., McQueeney, A.J., Ferrario, C.M. Brain Res. Bull. (1993) [Pubmed]
  24. The endothelium-dependent vasodilator effect of the nonpeptide Ang(1-7) mimic AVE 0991 is abolished in the aorta of mas-knockout mice. Lemos, V.S., Silva, D.M., Walther, T., Alenina, N., Bader, M., Santos, R.A. J. Cardiovasc. Pharmacol. (2005) [Pubmed]
  25. ANG II AT2 receptor modulates AT1 receptor-mediated descending vasa recta endothelial Ca2+ signaling. Rhinehart, K., Handelsman, C.A., Silldorff, E.P., Pallone, T.L. Am. J. Physiol. Heart Circ. Physiol. (2003) [Pubmed]
  26. Evidence that angiotensin-(1-7) plays a role in the central control of blood pressure at the ventro-lateral medulla acting through specific receptors. Fontes, M.A., Silva, L.C., Campagnole-Santos, M.J., Khosla, M.C., Guertzenstein, P.G., Santos, R.A. Brain Res. (1994) [Pubmed]
  27. Characterization of brain angiotensin II AT2 receptor subtype using [125I] CGP 42112A. Heemskerk, F.M., Zorad, S., Seltzer, A., Saavedra, J.M. Neuroreport (1993) [Pubmed]
  28. Effect of luminal angiotensin II receptor antagonists on proximal tubule transport. Quan, A., Baum, M. Am. J. Hypertens. (1999) [Pubmed]
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