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Chemical Compound Review

CHEMBL280822     2-hydroxy-5-[2-[[2-hydroxy-3- [4-[1-methyl...

Synonyms: AG-K-30350, CGP-20712, CGP-26505, SureCN10914264, CCG-204459, ...
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Disease relevance of CGP 20712A

  • 2. Sinoatrial tachycardia, evoked by (-)-adrenaline was resistant to blockade by beta(2)-selective ICI 118,551 (50 nM) but antagonized by beta(1)-selective CGP 20712A (300 nM) [1].
  • In left atria obtained from mice injected with 150 microg/kg i.p. pertussis toxin which abolished carbachol-evoked cardiode-pression, the positive inotropic effects of (-)-adrenaline were antagonised by CGP 20712A [2].

High impact information on CGP 20712A

  • When 300 nmol/L CGP 20712A was present as the sole antagonist, only a marginal shift of the concentration-response curve for (-)-epinephrine was usually observed, indicating that beta 1AR were not mediating the effect of these low concentrations of (-)-epinephrine [3].
  • Concentration-response curves to (-)-epinephrine were constructed in the presence and absence of selective antagonists for beta 1 AR (CGP 20712A) and beta 2 AR (ICI 118,551) [3].
  • The beta-adrenergic antagonists CGP 20712A (beta 1-selective) and ICI 118,551 (beta 2-selective) blocked in a dose-dependent fashion the ability of isoproterenol to effect receptor mRNA levels [4].
  • In contrast, beta2AR stimulation by zinterol or isoproterenol plus a selective beta1-adrenergic receptor (beta1AR) antagonist CGP 20712A failed to enhance the contractility in TG4 myocytes, and more surprisingly, beta2AR stimulation was also ineffective in increasing contractility in WT myocytes [5].
  • In the presence of CGP 20712A (beta 1-receptor blocker), a 100-fold higher concentration of zinterol increased the amplitude but prolonged the duration of the twitch in adult myocytes [6].

Chemical compound and disease context of CGP 20712A


Biological context of CGP 20712A


Anatomical context of CGP 20712A

  • Positive inotropic responses were established to (-)-isoprenaline, RO363 (beta 1-selective), procaterol (beta 2-selective) and dopexamine in the absence or presence of the antagonist CGP 20712A (beta 1-selective) or ICI 118,551 (beta 2-selective) in electrically driven human right atrial appendage strips [13].
  • In rat adipocyte membranes, displacement of [125I]ICYP by CGP 20712A and ICI 118,551 was biphasic, indicating high and low affinity sites; displacement profiles differed markedly between lumbar and parametrial depots, the former having a preponderance of beta 1-like receptors and the latter a preponderance of beta 2-like receptors [14].
  • 1. The nature of the beta-adrenoceptor(s) mediating adenylyl cyclase activation in rat adipocyte ghosts by (-)-isoprenaline and the lipolytically selective beta-adrenoceptor agonist, BRL 37344, was investigated by use of the beta 1-selective antagonist, CGP 20712A [15].
  • 4. The beta-AR agonist RO363 relaxed the ileum (pEC50=6.18) and was blocked by CGP20712A [16].
  • In plantaris muscle, monophasic competition curves were observed when binding experiments were performed using CGP20712A (50 pM to 0.5 mM), a beta 1-adrenoceptor selective antagonist, or ICI 118,551 (50 pM to 20 microM), a beta 2-adrenoceptor selective antagonist, to compete for ICYP binding [17].

Associations of CGP 20712A with other chemical compounds

  • This acidification, which was also observed in myocytes that were preloaded with the Ca2+ chelator BAPTA and superfused with nominally Ca(2+)-free solution, was blocked by propranolol as well as by the specific beta 1-antagonist CGP 20712 A but not by the beta 2-antagonist ICI 118,551 [18].
  • Among 11 beta antagonists tested, only ICI118551 and CGP20712A, previously classified as, respectively, beta 1 and beta 2 selective, inhibit this effect [19].
  • Inhibition of agonist-stimulated cyclic AMP production and competition binding experiments indicated that the beta 1-selective antagonists CGP 20712A and ICI 89,406 were much more potent than the beta 2-selective antagonist ICI 118,551 [20].
  • The apoptosis induced by the non-specific beta-AR agonist isoproterenol was largely blocked by the beta(1)-selective antagonist CGP 20712A, but not by the beta(2)-selective antagonist ICI 118551 [21].
  • Pharmacological tests showed that the beta(2)-adrenoceptor antagonist, ICI118,551, but not the beta(1)-adrenoceptor antagonist, CGP20712A, blocked the NE-induced IPSC facilitation, suggesting that the beta(2)-adrenoceptors on cerebellar interneurons, basket cells (BCs), mediate the noradrenergic facilitation of GABAergic transmission [22].

Gene context of CGP 20712A

  • Studies with CGP20712A or the beta 2AR-selective antagonist ICI118,551 indicated that this residual response was predominantly beta 2AR in character [23].
  • The pD(2) and pA(2) values of (-)-isoprenaline and CGP 20712A, respectively, were not different in left atria and right atria from mdx and C57 mice [24].
  • Iso stimulation at doses that reduced BNP mRNA expression increased TUNEL positive nuclei, an effect blocked by the beta1-antagonist CGP [25].
  • 3. Direct measurement of tissue radioactivity also showed that specific I-CYP binding was competitively inhibited in the presence of the beta-adrenoceptor antagonists (-)-propranolol (non-selective), CGP 20712A (beta 1-selective) and ICI 118,551 (beta 2-selective) [26].
  • 3. Increases of ventricular force by (-)-adrenaline and (-)-noradrenaline were not blocked by ICI 118,551 but antagonized by CGP 20712A [1].

Analytical, diagnostic and therapeutic context of CGP 20712A

  • We characterized beta-adrenoceptors in rat sinoatrial node (SA) and stellate ganglia by incubating consecutive tissue sections with [125I]iodocyanopindolol, with or without the beta 1-selective (CGP 20712A) or the beta 2-selective (ICI 118,551) antagonists, followed by quantitative autoradiography [27].


  1. Physiological antagonism between ventricular beta 1-adrenoceptors and alpha 1-adrenoceptors but no evidence for beta 2- and beta 3-adrenoceptor function in murine heart. Heubach, J.F., Rau, T., Eschenhagen, T., Ravens, U., Kaumann, A.J. Br. J. Pharmacol. (2002) [Pubmed]
  2. Pertussis toxin suppresses carbachol-evoked cardiodepression but does not modify cardiostimulation mediated through beta1- and putative beta4-adrenoceptors in mouse left atria: no evidence for beta2- and beta3-adrenoreceptor function. Oostendorp, J., Kaumann, A.J. Naunyn Schmiedebergs Arch. Pharmacol. (2000) [Pubmed]
  3. Coexistence of functioning beta 1- and beta 2-adrenoceptors in single myocytes from human ventricle. del Monte, F., Kaumann, A.J., Poole-Wilson, P.A., Wynne, D.G., Pepper, J., Harding, S.E. Circulation (1993) [Pubmed]
  4. Down-regulation of beta-adrenergic receptors: agonist-induced reduction in receptor mRNA levels. Hadcock, J.R., Malbon, C.C. Proc. Natl. Acad. Sci. U.S.A. (1988) [Pubmed]
  5. Coupling of beta2-adrenoceptor to Gi proteins and its physiological relevance in murine cardiac myocytes. Xiao, R.P., Avdonin, P., Zhou, Y.Y., Cheng, H., Akhter, S.A., Eschenhagen, T., Lefkowitz, R.J., Koch, W.J., Lakatta, E.G. Circ. Res. (1999) [Pubmed]
  6. Beta 2-adrenergic receptor actions in neonatal and adult rat ventricular myocytes. Kuznetsov, V., Pak, E., Robinson, R.B., Steinberg, S.F. Circ. Res. (1995) [Pubmed]
  7. Beta1-adrenoceptors in rat anterior pituitary may be constitutively active. Inverse agonism of CGP 20712A on basal 3',5'-cyclic adenosine 5'-monophosphate levels. Janssens, K., Boussemaere, M., Wagner, S., Kopka, K., Denef, C. Endocrinology (2008) [Pubmed]
  8. Subclassification of beta-adrenergic receptors of rat fat cells: a re-evaluation. Bahouth, S.W., Malbon, C.C. Mol. Pharmacol. (1988) [Pubmed]
  9. Characterisation of beta 1 and beta 2 adrenoceptor subtypes in the atrioventricular node of diabetic rat hearts by quantitative autoradiography. Saito, K., Kuroda, A., Tanaka, H. Cardiovasc. Res. (1991) [Pubmed]
  10. Chloride secretion by semicircular canal duct epithelium is stimulated via beta 2-adrenergic receptors. Milhaud, P.G., Pondugula, S.R., Lee, J.H., Herzog, M., Lehouelleur, J., Wangemann, P., Sans, A., Marcus, D.C. Am. J. Physiol., Cell Physiol. (2002) [Pubmed]
  11. Differential effects of epinephrine and norepinephrine on cAMP response and g(i3)alpha protein expression in cultured sympathetic neurons. Shivachar, A.C., Eikenburg, D.C. J. Pharmacol. Exp. Ther. (1999) [Pubmed]
  12. Beta 1- and beta 2-adrenoceptors in sheep cardiac ventricular muscle. Borea, P.A., Amerini, S., Masini, I., Cerbai, E., Ledda, F., Mantelli, L., Varani, K., Mugelli, A. J. Mol. Cell. Cardiol. (1992) [Pubmed]
  13. Coexistence and localization of beta 1- and beta 2-adrenoceptors in the human heart. Summers, R.J., Molnaar, P., Russell, F., Elnatan, J., Jones, C.R., Buxton, B.F., Chang, V., Hambley, J. Eur. Heart J. (1989) [Pubmed]
  14. Regional and interspecific differences in the ligand binding properties of beta-adrenergic receptors of individual white adipose tissue depots in the sheep and rat. Bowen, W.P., Flint, D.J., Vernon, R.G. Biochem. Pharmacol. (1992) [Pubmed]
  15. Relationship between lipolysis and cyclic AMP generation mediated by atypical beta-adrenoceptors in rat adipocytes. Hollenga, C., Brouwer, F., Zaagsma, J. Br. J. Pharmacol. (1991) [Pubmed]
  16. Characterization of beta-adrenoceptor mediated smooth muscle relaxation and the detection of mRNA for beta1-, beta2- and beta3-adrenoceptors in rat ileum. Roberts, S.J., Papaioannou, M., Evans, B.A., Summers, R.J. Br. J. Pharmacol. (1999) [Pubmed]
  17. Characterization of beta 1- and beta 2-adrenoceptors in rat skeletal muscles. Kim, Y.S., Sainz, R.D., Molenaar, P., Summers, R.J. Biochem. Pharmacol. (1991) [Pubmed]
  18. Chloride dependence of pH modulation by beta-adrenergic agonist in rat cardiomyocytes. Désilets, M., Pucéat, M., Vassort, G. Circ. Res. (1994) [Pubmed]
  19. The human beta 3-adrenergic receptor: relationship with atypical receptors. Emorine, L.J., Fève, B., Pairault, J., Briend-Sutren, M.M., Nahmias, C., Marullo, S., Delavier-Klutchko, C., Strosberg, D.A. Am. J. Clin. Nutr. (1992) [Pubmed]
  20. Characterization and regulation of beta 1-adrenergic receptors in a human neuroepithelioma cell line. Fishman, P.H., Nussbaum, E., Duman, R.S. J. Neurochem. (1991) [Pubmed]
  21. Subtype specific roles of beta-adrenergic receptors in apoptosis of adult rat ventricular myocytes. Shizukuda, Y., Buttrick, P.M. J. Mol. Cell. Cardiol. (2002) [Pubmed]
  22. beta-adrenergic receptor-mediated presynaptic facilitation of inhibitory GABAergic transmission at cerebellar interneuron-Purkinje cell synapses. Saitow, F., Satake, S., Yamada, J., Konishi, S. J. Neurophysiol. (2000) [Pubmed]
  23. Impaired expression and functional activity of the beta 3- and beta 1-adrenergic receptors in adipose tissue of congenitally obese (C57BL/6J ob/ob) mice. Collins, S., Daniel, K.W., Rohlfs, E.M., Ramkumar, V., Taylor, I.L., Gettys, T.W. Mol. Endocrinol. (1994) [Pubmed]
  24. Changes in function of cardiac receptors mediating the effects of the autonomic nervous system in the muscular dystrophy (MDX) mouse. Lu, S., Hoey, A. J. Mol. Cell. Cardiol. (2000) [Pubmed]
  25. Natriuretic peptide gene expression after beta-adrenergic stimulation in adult mouse cardiac myocytes. Ander, A.N., Duggirala, S.K., Drumm, J.D., Roth, D.M. DNA Cell Biol. (2004) [Pubmed]
  26. Distribution of beta 1- and beta 2-adrenoceptors in mouse trachea and lung: a quantitative autoradiographic study. Henry, P.J., Rigby, P.J., Goldie, R.G. Br. J. Pharmacol. (1990) [Pubmed]
  27. Characterization of beta 1- and beta 2-adrenoceptor subtypes in the rat sinoatrial node and stellate ganglia by quantitative autoradiography. Saito, K., Torda, T., Potter, W.Z., Saavedra, J.M. Neurosci. Lett. (1989) [Pubmed]
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