ICI 118,551 hydrochloride
Chemical Name: (±)-erythro-(S*,S*)-1-[2,3-(Dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanol hydrochloride
Biological ActivityVery selective β2 adrenergic 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™.
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.
Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the β2-adrenoceptor.
Bond et al.
β-Adrenoceptor subtypes and the opening of plasmalemmal K+-channels in trachealis muscle: electrophysiological and mechanical studies in guinea-pig tissue.
Cook et al.
The pharmacology of a β2-selective adrenoceptor antagonist (ICI-118,551).
Bilski et al.
Function and regulation of the β3-adrenoceptor.
Strosberg and Pietri-Rouxel
β2-but not β3-adrenoceptors mediate prejunctional inhibition of non-adrenergic non cholinergic contraction of guinea pig main bronchi.
Ten Berge et al.
Citations for ICI 118,551 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for ICI 118,551 hydrochloride include:
41 Citations: Showing 1 - 10
β2-adrenoreceptor Inverse Agonist Down-regulates Muscarine Cholinergic Subtype-3 Receptor and Its Downstream Signal Pathways in Airway Smooth Muscle Cells in vitro.
Scientific Reports 2017;7:39905
β2-adrenoreceptor stimulation dampens the LPS-induced M1 polarization in pig macrophages.
Dev Comp Immunol 2017;76:169
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
Adrenergic DNA damage of embryonic pluripotent cells via β2 receptor signalling.
Authors: Sun Et al.
J Pharmacol Exp Ther 2015;5:15950
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
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
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
β2-adrenoceptor signaling regulates invadopodia formation to enhance tumor cell invasion.
Authors: Creed Et al.
Breast Cancer Res 2015;17:145
Application of BRET to monitor ligand binding to GPCRs.
Authors: Stoddart Et al.
Nat Methods 2015;12:661
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
Galactomannan and Zymosan Block the Epinephrine-Induced Particle Transport in Tracheal Epithelium.
Authors: Weiterer Et al.
Circ Res 2015;10:e0143163
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
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
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
β2-Adrenergic receptor supports prolonged θ tetanus-induced LTP.
Authors: Qian Et al.
J Neurosci 2012;107:2703
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
CCK stimulation of GLP-1 neurons involves α1-adrenoceptor-mediated increase in glutamatergic synaptic inputs.
Authors: Hisadome Et al.
Effects of cholesterol depletion on compartmentalized cAMP responses in adult cardiac myocytes.
Authors: Agarwal Et al.
J Mol Cell Cardiol 2011;50:500
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
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
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.
Catecholamine up-regulates MMP-7 expression by activating AP-1 and STAT3 in gastric cancer.
Authors: Shi Et al.
PLoS Med 2010;9:269
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
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
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
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
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
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
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
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
Catechol-O-methyltransferase inhibition increases pain sensitivity through activation of both beta2- and beta3-adrenergic receptors.
Authors: Nackley Et al.
β 1-adrenergic receptor autoantibodies mediate dilated cardiomyopathy by agonistically inducing cardiomyocyte apoptosis.
Authors: Jane-Wit Et al.
Br J Pharmacol 2007;116:399
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
Central and peripheral components of the pressor effect of anandamide in urethane-anaesthetized rats.
Authors: Kwolek Et al.
Br J Pharmacol 2005;145:567
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
Noradrenergic inputs mediate state dependence of auditory responses in the avian song system.
Authors: Cardin and Schmidt
J Card Fail 2004;24:7745
Beta 2-adrenergic receptor regulation of human neutrophil function is sexually dimorphic.
Authors: Coupade Et al.
Br J Pharmacol 2004;143:1033
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
Nebivolol, bucindolol, metoprolol and carvedilol are devoid of intrinsic sympathomimetic activity in human myocardium.
Authors: Brixius Et al.
Br J Pharmacol 2001;133:1330
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
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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