ICI 118,551 hydrochloride

Cat. No. 0821

ICI 118,551 hydrochloride C17H27NO2.HCl [72795-01-8]

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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™.

Licensing Information

Sold with the permission of AstraZeneca UK Ltd.

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.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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.

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.

Bilski et al (1983) The pharmacology of a β2-selective adrenoceptor antagonist (ICI-118,551). J.Cardiovasc.Pharmacol. 5 430. PMID: 6191142.

If you know of a relevant reference for this product please let us know.

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

Creed et al (2015) β2-adrenoceptor signaling regulates invadopodia formation to enhance tumor cell invasion. Breast Cancer Res 17 145. PMID: 26607426.

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.

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.

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.

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.

Stoddart et al (2015) Application of BRET to monitor ligand binding to GPCRs. Nat Methods 12 661. PMID: 26030448.

Sun et al (2015) Adrenergic DNA damage of embryonic pluripotent cells via β2 receptor signalling. J Pharmacol Exp Ther 5 15950. PMID: 26516061.

Weiterer et al (2015) Galactomannan and Zymosan Block the Epinephrine-Induced Particle Transport in Tracheal Epithelium. Circ Res 10 e0143163. PMID: 26571499.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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

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.

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