ICI 118,551 hydrochloride

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Cat.No. 0821 - ICI 118,551 hydrochloride | C17H27NO2.HCl | CAS No. 72795-01-8
Description: Very selective β2 antagonist/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)
Datasheet
Citations (34)
Literature

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™.

Licensing Information

Sold with the permission of AstraZeneca UK Ltd.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 3.14 10
water 3.14 10

Preparing Stock Solutions

The following data is based on the product molecular weight 313.87. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.19 mL 15.93 mL 31.86 mL
5 mM 0.64 mL 3.19 mL 6.37 mL
10 mM 0.32 mL 1.59 mL 3.19 mL
50 mM 0.06 mL 0.32 mL 0.64 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


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34 Citations for ICI 118,551 hydrochloride

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

Qian et al (2012) β2-Adrenergic receptor supports prolonged θ tetanus-induced LTP. J Neurosci 107 2703 PMID: 22338020

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

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

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

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

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

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

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

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

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

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

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

Coupade et al (2004) Beta 2-adrenergic receptor regulation of human neutrophil function is sexually dimorphic. Br J Pharmacol 143 1033 PMID: 15477226

Cardin and Schmidt (2004) Noradrenergic inputs mediate state dependence of auditory responses in the avian song system. J Card Fail 24 7745 PMID: 15342742

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

Brixius et al (2001) Nebivolol, bucindolol, metoprolol and carvedilol 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

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

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

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

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

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

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


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