Catalog Number: 1024
Chemical Name: 1-[2-((3-Carbamoyl-4-hydroxy)phenoxy)ethylamino]-3-[4-(1-methyl-4-trifluoromethyl-2-imidazolyl)phenoxy]-2-propanol dihydrochloride
Biological Activity
Highly selective and potent β1-adrenoceptor antagonist (IC50 = 0.7 nM). Displays 10,000-fold selectivity over β2-adrenoceptors. Also available as part of the β-Adrenoceptor Antagonist Tocriset™.
Technical Data
  • M.Wt:
    567.39
  • Formula:
    C23H25F3N4O5.2HCl
  • Solubility:
    Soluble to 50 mM in water
  • Purity:
    >96%
  • Storage:
    Desiccate at +4°C
  • CAS No:
    1216905-73-5
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. β- and γ-Adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
    Hieble et al.
    J.Med.Chem., 1995;38:3415
  2. CGP 20712A: a useful tool for quantitating β1- and β2-adrenoceptors.
    Dooley et al.
    Eur.J.Pharmacol., 1986;130:137
  3. Determination of β-adrenoceptor subtype on rat isolated ventricular myocytes by use of highly selective β-antagonists.
    Kitagawa et al.
    Br.J.Pharmacol., 1995;116:1635
Citations:

The citations listed below are publications that use Tocris products. Selected citations for CGP 20712 dihydrochloride include:

15 Citations: Showing 1 - 10
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  1. β2-Adrenergic Receptor Antagonism Attenuates CNV Through Inhibition of VEGF and IL-6 Expression.
    Authors: Lavine
    Invest Ophthalmol Vis Sci 2017;58(1):299
  2. Recruitment of β-arrestin 1 and 2 to the β2-adrenoceptor: analysis of 65 ligands.
    Authors: Littmann Et al.
    J Biol Chem 2015;355:183
  3. β2-adrenoceptor signaling regulates invadopodia formation to enhance tumor cell invasion.
    Authors: Creed Et al.
    Breast Cancer Res 2015;17:145
  4. Galactomannan and Zymosan Block the Epinephrine-Induced Particle Transport in Tracheal Epithelium.
    Authors: Weiterer Et al.
    J Neurochem 2015;10:e0143163
  5. Detection of the secondary, low-affinity β1 -adrenoceptor site in living cells using the fluorescent CGP 12177 derivative BODIPY-TMR-CGP.
    Authors: Gherbi Et al.
    Br J Pharmacol 2014;171:5431
  6. Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.
    Authors: Mistry Et al.
    J Med Chem 2013;56:3852
  7. Attenuation of choroidal neovascularization by β(2)-adrenoreceptor antagonism.
    Authors: Lavine Et al.
    JAMA Ophthalmol 2013;131:376
  8. Cardiovascular agents affect the tone of pulmonary arteries and veins in precision-cut lung slices.
    Authors: Rieg Et al.
    PLoS One 2012;6:e29698
  9. Cytoskeletal role in protection of the failing heart by β-adrenergic blockade.
    Authors: Cheng Et al.
    Am J Physiol Heart Circ Physiol 2012;302:H675
  10. Both α1- and β1-adrenoceptors in the bed nucleus of the stria terminalis are involved in the expression of conditioned contextual fear.
    Authors: Hott Et al.
    Br J Pharmacol 2012;167:207
  11. Modulation of calcium-dependent inactivation of L-type Ca2+ channels via β-adrenergic signaling in thalamocortical relay neurons.
    Authors: Rankovic Et al.
    PLoS One 2011;6:e27474
  12. β-Adrenergic receptor stimulation and activation of protein kinase A protect against α1-adrenergic-mediated phosphorylation of protein kinase D and histone deacetylase 5.
    Authors: Sucharov Et al.
    Circulation 2011;17:592
  13. Unchanged β-adrenergic stimulation of cardiac L-type calcium channels in Ca v 1.2 phosphorylation site S1928A mutant mice.
    Authors: Lemke Et al.
    PLoS One 2008;283:34738
  14. Both alpha1 and alpha2-adrenoceptors mediate the cardiovascular responses to noradrenaline microinjected into the bed nucleus of the stria terminal of rats.
    Authors: Crestani Et al.
    Br J Pharmacol 2008;153:583
  15. β 1-adrenergic receptor autoantibodies mediate dilated cardiomyopathy by agonistically inducing cardiomyocyte apoptosis.
    Authors: Jane-Wit Et al.
    J Pharmacol Exp Ther 2007;116:399
Expand to show all 15 Citations

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