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Submit ReviewICI 118,551 hydrochloride
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% (HPLC)
Biological Activity for ICI 118,551 hydrochloride
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.
Licensing Information
Sold with the permission of AstraZeneca UK Ltd.
Technical Data for ICI 118,551 hydrochloride
| M. Wt | 313.87 |
| Formula | C17H27NO2.HCl |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 72795-01-8 |
| PubChem ID | 46704341 |
| InChI Key | KBXMBGWSOLBOQM-MELYUZJYSA-N |
| Smiles | CC1=C(CCC2)C2=C(OC[C@@H](O)[C@H](C)NC(C)C)C=C1.Cl |
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.
Solubility Data for ICI 118,551 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 3.14 | 10 | |
| water | 3.14 | 10 |
Preparing Stock Solutions for ICI 118,551 hydrochloride
The following data is based on the product molecular weight 313.87. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 31.86 mL | 159.3 mL | 318.6 mL |
| 0.5 mM | 6.37 mL | 31.86 mL | 63.72 mL |
| 1 mM | 3.19 mL | 15.93 mL | 31.86 mL |
| 5 mM | 0.64 mL | 3.19 mL | 6.37 mL |
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Product Datasheets for ICI 118,551 hydrochloride
References for ICI 118,551 hydrochloride
References are publications that support the biological activity of the product.
Bilski et al (1983) The pharmacology of a β2-selective adrenoceptor antagonist (ICI-118,551). J.Cardiovasc.Pharmacol. 5 430 PMID: 6191142
Cook et al (1993) β-Adrenoceptor subtypes and the opening of plasmalemmal K+-channels in trachealis muscle: electrophysiological and mechanical studies in guinea-pig tissue. Br.J.Pharmacol. 109 1140 PMID: 8104643
Strosberg and Pietri-Rouxel (1996) Function and regulation of the β3-adrenoceptor. TiPS 17 373 PMID: 8979772
Ten Berge et al (1995) β2-but not β3-adrenoceptors mediate prejunctional inhibition of non-adrenergic non cholinergic contraction of guinea pig main bronchi. Eur.J.Pharmacol. 275 199 PMID: 7796855
Bond et al (1995) Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the β2-adrenoceptor. Nature 374 272 PMID: 7885448
If you know of a relevant reference for ICI 118,551 hydrochloride, please let us know.
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45 Citations for ICI 118,551 hydrochloride
Citations are publications that use Tocris products. Selected citations for ICI 118,551 hydrochloride include:
Gill et al (2016) Evaluation of the anti-inflammatory effects of β-adrenoceptor agonists on human lung macrophages European Journal of Pharmacology 793 49 PMID: 27832943
Hott et al (2012) Both α1- and β1-adrenoceptors in the bed nucleus of the stria terminalis are involved in the expression of conditioned contextual fear. Br J Pharmacol 167 207 PMID: 22506532
Cheng et al (2012) Cytoskeletal role in protection of the failing heart by β-adrenergic blockade. Am J Physiol Heart Circ Physiol 302 H675 PMID: 22081703
Shi et al (2010) Catecholamine up-regulates MMP-7 expression by activating AP-1 and STAT3 in gastric cancer. PLoS Med 9 269 PMID: 20939893
Brinks et al (2010) Level of G protein-coupled receptor kinase-2 determines myocardial ischemia/reperfusion injury via pro- and anti-apoptotic mechanisms. J Pharmacol Exp Ther 107 1140 PMID: 20814022
Zhang et al (2018) Androgen deprivation promotes neuroendocrine differentiation and angiogenesis through CREB-EZH2-TSP1 pathway in prostate cancers. Nat Commun 9 4080 PMID: 30287808
Lucido et al (2018) β2-Adrenergic receptor modulates mitochondrial metabolism and disease progression in recurrent/metastatic HPV(+) HNSCC. Oncogenesis 7 81 PMID: 30297705
Qian et al (2012) β2-Adrenergic receptor supports prolonged θ tetanus-induced LTP. J Neurosci 107 2703 PMID: 22338020
Sucharov et al (2011) β-Adrenergic receptor stimulation and activation of protein kinase A protect against α1-adrenergic-mediated phosphorylation of protein kinase D and histone deacetylase 5. Circulation 17 592 PMID: 21703532
Creed et al (2015) β2-adrenoceptor signaling regulates invadopodia formation to enhance tumor cell invasion. Breast Cancer Res 17 145 PMID: 26607426
Stoddart et al (2015) Application of BRET to monitor ligand binding to GPCRs. Nat Methods 12 661 PMID: 26030448
Rankovic et al (2011) Modulation of calcium-dependent inactivation of L-type Ca2+ channels via β-adrenergic signaling in thalamocortical relay neurons. PLoS One 6 e27474 PMID: 22164209
Komolov et al (2017) Structural and Functional Analysis of a β2-Adrenergic Receptor Complex with GRK5. Cell 169 407 PMID: 28431242
Dasu et al (2014) Crosstalk between adrenergic and toll-like receptors in human mesenchymal stem cells and keratinocytes: a recipe for impaired wound healing. Stem Cells Transl Med 3 745 PMID: 24760207
Kaya et al (2009) Coupling of β2-adrenoceptors to XLαs and Gαs: a new insight into ligand-induced G protein activation. PLoS One 329 350 PMID: 19144685
Sivamani et al (2009) Stress-mediated increases in systemic and local epinephrine impair skin wound healing: potential new indication for β blockers. Circ Res 6 e12 PMID: 19143471
Lemke et al (2008) Unchanged β-adrenergic stimulation of cardiac L-type calcium channels in Ca v 1.2 phosphorylation site S1928A mutant mice. Mol Cancer 283 34738 PMID: 18829456
Desantiago et al (2008) Arrhythmogenic effects of β2-adrenergic stimulation in the failing heart are attributable to enhanced sarcoplasmic reticulum Ca load. Am J Physiol Cell Physiol 102 1389 PMID: 18467626
Crestani et al (2008) Both alpha1 and alpha2-adrenoceptors mediate the cardiovascular responses to noradrenaline microinjected into the bed nucleus of the stria terminal of rats. Br J Pharmacol 153 583 PMID: 18037912
Kilpatrick et al (2019) Complex Formation between VEGFR2 and the β2-Adrenoceptor. Cell Chem Biol PMID: 30956148
Agarwal et al (2011) Effects of cholesterol depletion on compartmentalized cAMP responses in adult cardiac myocytes. J Mol Cell Cardiol 50 500 PMID: 21115018
Schutsky et al (2011) Stress and glucocorticoids impair memory retrieval via β2-adrenergic, Gi/o-coupled suppression of cAMP signaling. J Neurosci 31 14172 PMID: 21976502
Hisadome et al (2011) CCK stimulation of GLP-1 neurons involves α1-adrenoceptor-mediated increase in glutamatergic synaptic inputs. Diabetes 60 2701 PMID: 21885869
Chigaev et al (2011) Real-time analysis of the inside-out regulation of lymphocyte function-associated antigen-1 revealed similarities to and differences from very late antigen-4. J Biol Chem 286 20375 PMID: 21515675
Scola et al (2009) The long-acting beta-adrenoceptor agonist, indacaterol, inhibits IgE-dependent responses of human lung mast cells. Br J Pharmacol 158 267 PMID: 19371332
Bacou (2017) β2-adrenoreceptor stimulation dampens the LPS-induced M1 polarization in pig macrophages. Dev Comp Immunol 76 169 PMID: 28633932
Luo (2017) 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 7 39905 PMID: 28051147
Weiterer et al (2015) Galactomannan and Zymosan Block the Epinephrine-Induced Particle Transport in Tracheal Epithelium. Circ Res 10 e0143163 PMID: 26571499
Liu et al (2015) 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. Sci Rep 11 4121 PMID: 25672589
Sun et al (2015) Adrenergic DNA damage of embryonic pluripotent cells via β2 receptor signalling. J Pharmacol Exp Ther 5 15950 PMID: 26516061
Littmann et al (2015) Recruitment of β-arrestin 1 and 2 to the β2-adrenoceptor: analysis of 65 ligands. Pharmacol Res Perspect 355 183 PMID: 26306764
Pecha et al (2015) 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. J Sleep Res 3 e00168 PMID: 26516580
Kim et al (2015) Chronic sleep restriction induces long-lasting changes in adenosine and noradrenaline receptor density in the rat brain. J Biol Chem 24 549 PMID: 25900125
Heubach et al (2001) 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. Br J Pharmacol 133 73 PMID: 11325796
Brixius et al (2001) Nebivolol, bucindolol, metop. and carve. are devoid of intrinsic sympathomimetic activity in human myocardium. Br J Pharmacol 133 1330 PMID: 11498519
Nagaraja et al (1999) Treatment with inverse agonists enhances baseline atrial contractility in transgenic mice with chronic β2-adrenoceptor activation. Mol Med Rep 127 1099 PMID: 10455254
Skeberdis et al (1997) Pharmacological characterization of the receptors involved in the beta-adrenoceptor-mediated stimulation of the L-type Ca2+ current in frog ventricular myocytes. Br J Pharmacol 121 1277 PMID: 9257904
Cardin and Schmidt (2004) Noradrenergic inputs mediate state dependence of auditory responses in the avian song system. J Card Fail 24 7745 PMID: 15342742
Kwolek et al (2005) Central and peripheral components of the pressor effect of anandamide in urethane-anaesthetized rats. Br J Pharmacol 145 567 PMID: 15834445
Chanrachakul et al (2004) Contribution of coupling between human myometrial β2-adrenoreceptor and the BK(Ca) channel to uterine quiescence. Br J Pharmacol 287 C1747 PMID: 15329337
Coupade et al (2004) Beta 2-adrenergic receptor regulation of human neutrophil function is sexually dimorphic. Br J Pharmacol 143 1033 PMID: 15477226
Hucho et al (2005) Epac mediates a cAMP-to-PKC signaling in inflammatory pain: an isolectin B4(+) neuron-specific mechanism. J Neurosci 25 6119 PMID: 15987941
Maupoil et al (2007) Ectopic activity in the rat pulmonary vein can arise from simultaneous activation of alpha1- and beta1-adrenoceptors. Br J Pharmacol 150 899 PMID: 17325650
Jane-Wit et al (2007) β 1-adrenergic receptor autoantibodies mediate dilated cardiomyopathy by agonistically inducing cardiomyocyte apoptosis. Br J Pharmacol 116 399 PMID: 17620508
Nackley et al (2007) Catechol-O-methyltransferase inhibition increases pain sensitivity through activation of both beta2- and beta3-adrenergic receptors. Pain 128 199 PMID: 17084978
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