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 (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:
  • Formula:
  • Solubility:
    Soluble to 10 mM in DMSO and to 10 mM in water
  • Purity:
  • Storage:
    Store at RT
  • CAS No:
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

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

Showing Results 1 - 10 of 31

  1. Adrenergic DNA damage of embryonic pluripotent cells via β2 receptor signalling.
    Authors: Sun Et al.
    J Pharmacol Exp Ther
  2. 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
  3. Recruitment of β-arrestin 1 and 2 to the β2-adrenoceptor: analysis of 65 ligands.
    Authors: Littmann Et al.
    Pharmacol Res Perspect
  4. Chronic sleep restriction induces long-lasting changes in adenosine and noradrenaline receptor density in the rat brain.
    Authors: Kim Et al.
    J Biol Chem
  5. β2-adrenoceptor signaling regulates invadopodia formation to enhance tumor cell invasion.
    Authors: Creed Et al.
    Breast Cancer Res
  6. Application of BRET to monitor ligand binding to GPCRs.
    Authors: Stoddart Et al.
    Nat Methods
  7. 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
  8. Galactomannan and Zymosan Block the Epinephrine-Induced Particle Transport in Tracheal Epithelium.
    Authors: Weiterer Et al.
    Circ Res
  9. 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
  10. Cytoskeletal role in protection of the failing heart by β-adrenergic blockade.
    Authors: Cheng Et al.
    Am J Physiol Heart Circ Physiol
  11. 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
  12. β2-Adrenergic receptor supports prolonged θ tetanus-induced LTP.
    Authors: Qian Et al.
    J Neurosci
  13. Modulation of calcium-dependent inactivation of L-type Ca2+ channels via β-adrenergic signaling in thalamocortical relay neurons.
    Authors: Rankovic Et al.
    PLoS One
  14. 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.
  15. Catecholamine up-regulates MMP-7 expression by activating AP-1 and STAT3 in gastric cancer.
    Authors: Shi Et al.
    PLoS Med
  16. 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
  17. Stress-mediated increases in systemic and local epinephrine impair skin wound healing: potential new indication for β blockers.
    Authors: Sivamani Et al.
    Circ Res
  18. Coupling of β2-adrenoceptors to XLαs and Gαs: a new insight into ligand-induced G protein activation.
    Authors: Kaya Et al.
    PLoS One
  19. The long-acting beta-adrenoceptor agonist, indacaterol, inhibits IgE-dependent responses of human lung mast cells.
    Authors: Scola Et al.
    Br J Pharmacol
  20. 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
  21. 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
  22. 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
  23. Ectopic activity in the rat pulmonary vein can arise from simultaneous activation of alpha1- and beta1-adrenoceptors.
    Authors: Maupoil Et al.
    Br J Pharmacol
  24. β 1-adrenergic receptor autoantibodies mediate dilated cardiomyopathy by agonistically inducing cardiomyocyte apoptosis.
    Authors: Jane-Wit Et al.
    Br J Pharmacol
  25. Central and peripheral components of the pressor effect of anandamide in urethane-anaesthetized rats.
    Authors: Kwolek Et al.
    Br J Pharmacol
  26. Contribution of coupling between human myometrial β2-adrenoreceptor and the BK(Ca) channel to uterine quiescence.
    Authors: Chanrachakul Et al.
    Br J Pharmacol
  27. Noradrenergic inputs mediate state dependence of auditory responses in the avian song system.
    Authors: Cardin and Schmidt
    J Card Fail
  28. Beta 2-adrenergic receptor regulation of human neutrophil function is sexually dimorphic.
    Authors: Coupade Et al.
    Br J Pharmacol
  29. Nebivolol, bucindolol, metoprolol and carvedilol are devoid of intrinsic sympathomimetic activity in human myocardium.
    Authors: Brixius Et al.
    Br J Pharmacol
  30. Treatment with inverse agonists enhances baseline atrial contractility in transgenic mice with chronic β2-adrenoceptor activation.
    Authors: Nagaraja Et al.
    Mol Med Rep
  31. 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
Expand to show all
Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.

Order Details


Contact Information

Molarity Calculator
Calculate the mass, volume or concentration required for a solution

The molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) x Volume (L) x Molecular Weight (g/mol)
An example of a molarity calculation using the molarity calculator:
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?

R&D Systems Guarantee

or select another batch:


Customer Information