Home / Adrenergic beta 2 Receptor Inverse Agonists / ICI 118,551 hydrochloride

ICI 118,551 hydrochloride

Catalog #: 0821
45 Citations Datasheet / COA / SDS
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0821/50
ICI 118,551 hydrochloride | CAS No. 72795-01-8 | Adrenergic beta 2 Receptor Inverse Agonists
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Description: Highly selective β2 inverse agonist

Chemical Name: (±)-erythro-(S*,S*)-1-[2,3-(Dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanol hydrochloride

Purity: ≥98%

Product Details
Citations (45)
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Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

ICI 118,551 hydrochloride is a very selective β2 adrenergic inverse agonist (Ki values are 1.2, 120 and 257 nM for β2, β1 and β3 receptors respectively). Active in vivo.

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold with the permission of AstraZeneca UK Ltd.

Background References

  1. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
    Fox JT, Sakamuru S, Huang R
    Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
  2. Role of AKAP79/150 protein in beta1-adrenergic receptor trafficking and signaling in mammalian cells.
    Li X, Nooh M, Bahouth S
    J Biol Chem, 2013;288(47):33797-812.
  3. Protein kinase A activation inhibits DUX4 gene expression in myotubes from patients with facioscapulohumeral muscular dystrophy
    JM Cruz, N Hupper, LS Wilson, JB Concannon, Y Wang, B Oberhauser, K Patora-Kom, Y Zhang, DJ Glass, AU Trendelenb, BA Clarke
    J. Biol. Chem., 2018;0(0):.
  4. Activation of ?2A-adrenergic signal transduction in chondrocytes promotes degenerative remodelling of temporomandibular joint

    Sci Rep, 2016;6(0):30085.
  5. Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the β2-adrenoceptor.
    Bond et al.
    Nature, 1995;374:272
  6. The pharmacology of a β2-selective adrenoceptor antagonist (ICI-118,551).
    Bilski et al.
    J.Cardiovasc.Pharmacol., 1983;5:430
  7. 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
  8. Function and regulation of the β3-adrenoceptor.
    Strosberg and Pietri-Rouxel
    TiPS, 1996;17:373
  9. 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
  10. Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the β2-adrenoceptor.
    Bond et al.
    Nature, 1995;374:272

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Citations for ICI 118,551 hydrochloride

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

45 Citations: Showing 1 - 10

  1. Complex Formation between VEGFR2 and the β2-Adrenoceptor.
    Authors: Kilpatrick Et al.
    Cell Chem Biol  2019;
  2. Androgen deprivation promotes neuroendocrine differentiation and angiogenesis through CREB-EZH2-TSP1 pathway in prostate cancers.
    Authors: Zhang Et al.
    Nat Commun  2018;9:4080
  3. β2-Adrenergic receptor modulates mitochondrial metabolism and disease progression in recurrent/metastatic HPV(+) HNSCC.
    Authors: Lucido Et al.
    Oncogenesis  2018;7:81
  4. 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
  5. β2-adrenoreceptor stimulation dampens the LPS-induced M1 polarization in pig macrophages.
    Authors: Bacou
    Dev Comp Immunol  2017;76:169
  6. Structural and Functional Analysis of a β2-Adrenergic Receptor Complex with GRK5.
    Authors: Komolov Et al.
    Cell  2017;169:407
  7. 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
  8. Adrenergic DNA damage of embryonic pluripotent cells via β2 receptor signalling.
    Authors: Sun Et al.
    J Pharmacol Exp Ther  2015;5:15950
  9. 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
  10. 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
  11. 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
  12. β2-adrenoceptor signaling regulates invadopodia formation to enhance tumor cell invasion.
    Authors: Creed Et al.
    Breast Cancer Res  2015;17:145
  13. Application of BRET to monitor ligand binding to GPCRs.
    Authors: Stoddart Et al.
    Nat Methods  2015;12:661
  14. 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
  15. Galactomannan and Zymosan Block the Epinephrine-Induced Particle Transport in Tracheal Epithelium.
    Authors: Weiterer Et al.
    Circ Res  2015;10:e0143163
  16. 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
  17. 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
  18. 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
  19. β2-Adrenergic receptor supports prolonged θ tetanus-induced LTP.
    Authors: Qian Et al.
    J Neurosci  2012;107:2703
  20. 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
  21. CCK stimulation of GLP-1 neurons involves α1-adrenoceptor-mediated increase in glutamatergic synaptic inputs.
    Authors: Hisadome Et al.
    Diabetes  2011;60:2701
  22. Effects of cholesterol depletion on compartmentalized cAMP responses in adult cardiac myocytes.
    Authors: Agarwal Et al.
    J Mol Cell Cardiol  2011;50:500
  23. Stress and glucocorticoids impair memory retrieval via β2-adrenergic, Gi/o-coupled suppression of cAMP signaling.
    Authors: Schutsky Et al.
    J Neurosci  2011;31:14172
  24. Real-time analysis of the inside-out regulation of lymphocyte function-associated antigen-1 revealed similarities to and differences from very late antigen-4.
    Authors: Chigaev Et al.
    J Biol Chem  2011;286:20375
  25. 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
  26. Catecholamine up-regulates MMP-7 expression by activating AP-1 and STAT3 in gastric cancer.
    Authors: Shi Et al.
    PLoS Med  2010;9:269
  27. 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
  28. 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
  29. 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
  30. 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
  31. 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
  32. 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
  33. 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
  34. 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
  35. Catechol-O-methyltransferase inhibition increases pain sensitivity through activation of both beta2- and beta3-adrenergic receptors.
    Authors: Nackley Et al.
    Pain  2007;128:199
  36. β 1-adrenergic receptor autoantibodies mediate dilated cardiomyopathy by agonistically inducing cardiomyocyte apoptosis.
    Authors: Jane-Wit Et al.
    Br J Pharmacol  2007;116:399
  37. Epac mediates a cAMP-to-PKC signaling in inflammatory pain: an isolectin B4(+) neuron-specific mechanism.
    Authors: Hucho Et al.
    J Neurosci  2005;25:6119
  38. Central and peripheral components of the pressor effect of anandamide in urethane-anaesthetized rats.
    Authors: Kwolek Et al.
    Br J Pharmacol  2005;145:567
  39. 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
  40. Noradrenergic inputs mediate state dependence of auditory responses in the avian song system.
    Authors: Cardin and Schmidt
    J Card Fail  2004;24:7745
  41. Beta 2-adrenergic receptor regulation of human neutrophil function is sexually dimorphic.
    Authors: Coupade Et al.
    Br J Pharmacol  2004;143:1033
  42. Murine ventricular L-type Ca(2+) current is enhanced by zinterol via beta(1)-adrenoceptors, and is reduced in TG4 mice overexpressing the human beta(2)-adrenoceptor.
    Authors: Heubach Et al.
    Br J Pharmacol  2001;133:73
  43. Nebivolol, bucindolol, metop. and carve. are devoid of intrinsic sympathomimetic activity in human myocardium.
    Authors: Brixius Et al.
    Br J Pharmacol  2001;133:1330
  44. 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
  45. 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

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