Catalog Number: 0821
Chemical Name: (±)-erythro-(S*,S*)-1-[2,3-(Dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanol hydrochloride
Biological Activity
Very selective β2 adrenergic antagonist/inverse agonist (Ki values are 1.2, 120 and 257 nM for β2, β1 and β3 receptors respectively). Active in vivo. Also available as part of the β-Adrenoceptor Antagonist Tocriset™.
Technical Data
  • M.Wt:
    313.87
  • Formula:
    C17H27NO2.HCl
  • Solubility:
    Soluble to 10 mM in DMSO and to 10 mM in water
  • Purity:
    >98%
  • Storage:
    Store at RT
  • CAS No:
    72795-01-8
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.
Additional Information
Licensing Caveats:
Sold with the permission of AstraZeneca UK Ltd.
Background References
  1. Function and regulation of the β3-adrenoceptor.
    Strosberg and Pietri-Rouxel
    TiPS, 1996;17:373
  2. The pharmacology of a β2-selective adrenoceptor antagonist (ICI-118,551).
    Bilski et al.
    J.Cardiovasc.Pharmacol., 1983;5:430
  3. β-Adrenoceptor subtypes and the opening of plasmalemmal K+-channels in trachealis muscle: electrophysiological and mechanical studies in guinea-pig tissue.
    Cook et al.
    Br.J.Pharmacol., 1993;109:1140
  4. β2-but not β3-adrenoceptors mediate prejunctional inhibition of non-adrenergic non cholinergic contraction of guinea pig main bronchi.
    Ten Berge et al.
    Eur.J.Pharmacol., 1995;275:199
Citations:

The citations listed below are publications that use Tocris products. Selected citations for ICI 118,551 hydrochloride include:

34 Citations: Showing 1 - 10
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  1. β2-adrenoreceptor Inverse Agonist Down-regulates Muscarine Cholinergic Subtype-3 Receptor and Its Downstream Signal Pathways in Airway Smooth Muscle Cells in vitro.
    Authors: Luo
    Scientific Reports 2017;7:39905
  2. β2-adrenoreceptor stimulation dampens the LPS-induced M1 polarization in pig macrophages.
    Authors: Bacou
    Dev Comp Immunol 2017;76:169
  3. Evaluation of the anti-inflammatory effects of β-adrenoceptor agonists on human lung macrophages
    Authors: Gill Et al.
    European Journal of Pharmacology 2016;793:49
  4. Adrenergic DNA damage of embryonic pluripotent cells via β2 receptor signalling.
    Authors: Sun Et al.
    J Pharmacol Exp Ther 2015;5:15950
  5. β 1 Adrenoceptor antagonistic effects of the supposedly selective β 2 adrenoceptor antagonist ICI 118,551 on the positive inotropic effect of adrenaline in murine hearts.
    Authors: Pecha Et al.
    J Sleep Res 2015;3:e00168
  6. Recruitment of β-arrestin 1 and 2 to the β2-adrenoceptor: analysis of 65 ligands.
    Authors: Littmann Et al.
    Pharmacol Res Perspect 2015;355:183
  7. Chronic sleep restriction induces long-lasting changes in adenosine and noradrenaline receptor density in the rat brain.
    Authors: Kim Et al.
    J Biol Chem 2015;24:549
  8. β2-adrenoceptor signaling regulates invadopodia formation to enhance tumor cell invasion.
    Authors: Creed Et al.
    Breast Cancer Res 2015;17:145
  9. Application of BRET to monitor ligand binding to GPCRs.
    Authors: Stoddart Et al.
    Nat Methods 2015;12:661
  10. A long-acting β2-adrenergic agonist increases the expression of muscarine cholinergic subtype-3 receptors by activating the β2-adrenoceptor cyclic adenosine monophosphate signaling pathway in airway smooth muscle cells.
    Authors: Liu Et al.
    Sci Rep 2015;11:4121
  11. Galactomannan and Zymosan Block the Epinephrine-Induced Particle Transport in Tracheal Epithelium.
    Authors: Weiterer Et al.
    Circ Res 2015;10:e0143163
  12. Crosstalk between adrenergic and toll-like receptors in human mesenchymal stem cells and keratinocytes: a recipe for impaired wound healing.
    Authors: Dasu Et al.
    Stem Cells Transl Med 2014;3:745
  13. 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
  14. 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
  15. β2-Adrenergic receptor supports prolonged θ tetanus-induced LTP.
    Authors: Qian Et al.
    J Neurosci 2012;107:2703
  16. 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
  17. 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
  18. Catecholamine up-regulates MMP-7 expression by activating AP-1 and STAT3 in gastric cancer.
    Authors: Shi Et al.
    PLoS Med 2010;9:269
  19. Level of G protein-coupled receptor kinase-2 determines myocardial ischemia/reperfusion injury via pro- and anti-apoptotic mechanisms.
    Authors: Brinks Et al.
    J Pharmacol Exp Ther 2010;107:1140
  20. Stress-mediated increases in systemic and local epinephrine impair skin wound healing: potential new indication for β blockers.
    Authors: Sivamani Et al.
    Circ Res 2009;6:e12
  21. Coupling of β2-adrenoceptors to XLαs and Gαs: a new insight into ligand-induced G protein activation.
    Authors: Kaya Et al.
    PLoS One 2009;329:350
  22. The long-acting beta-adrenoceptor agonist, indacaterol, inhibits IgE-dependent responses of human lung mast cells.
    Authors: Scola Et al.
    Br J Pharmacol 2009;158:267
  23. Unchanged β-adrenergic stimulation of cardiac L-type calcium channels in Ca v 1.2 phosphorylation site S1928A mutant mice.
    Authors: Lemke Et al.
    Mol Cancer 2008;283:34738
  24. 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
  25. Arrhythmogenic effects of β2-adrenergic stimulation in the failing heart are attributable to enhanced sarcoplasmic reticulum Ca load.
    Authors: Desantiago Et al.
    Am J Physiol Cell Physiol 2008;102:1389
  26. Ectopic activity in the rat pulmonary vein can arise from simultaneous activation of alpha1- and beta1-adrenoceptors.
    Authors: Maupoil Et al.
    Br J Pharmacol 2007;150:899
  27. β 1-adrenergic receptor autoantibodies mediate dilated cardiomyopathy by agonistically inducing cardiomyocyte apoptosis.
    Authors: Jane-Wit Et al.
    Br J Pharmacol 2007;116:399
  28. Central and peripheral components of the pressor effect of anandamide in urethane-anaesthetized rats.
    Authors: Kwolek Et al.
    Br J Pharmacol 2005;145:567
  29. Contribution of coupling between human myometrial β2-adrenoreceptor and the BK(Ca) channel to uterine quiescence.
    Authors: Chanrachakul Et al.
    Br J Pharmacol 2004;287:C1747
  30. Noradrenergic inputs mediate state dependence of auditory responses in the avian song system.
    Authors: Cardin and Schmidt
    J Card Fail 2004;24:7745
  31. Beta 2-adrenergic receptor regulation of human neutrophil function is sexually dimorphic.
    Authors: Coupade Et al.
    Br J Pharmacol 2004;143:1033
  32. Nebivolol, bucindolol, metoprolol and carvedilol are devoid of intrinsic sympathomimetic activity in human myocardium.
    Authors: Brixius Et al.
    Br J Pharmacol 2001;133:1330
  33. Treatment with inverse agonists enhances baseline atrial contractility in transgenic mice with chronic β2-adrenoceptor activation.
    Authors: Nagaraja Et al.
    Mol Med Rep 1999;127:1099
  34. Pharmacological characterization of the receptors involved in the beta-adrenoceptor-mediated stimulation of the L-type Ca2+ current in frog ventricular myocytes.
    Authors: Skeberdis Et al.
    Br J Pharmacol 1997;121:1277
Expand to show all 34 Citations

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