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Biological Activity for Formoterol hemifumarate
Formoterol hemifumarate is a potent, selective and long-acting β2-adrenoceptor agonist. Displays 330-fold selectivity for β2 over β1 receptors (pKd values are 8.12 and 5.58 respectively). Potently relaxes guinea pig trachea (pD2 = 9.29), and is longer-acting and 100-fold more potent than Salbutamol (Cat. No. 0634).
Compound Libraries for Formoterol hemifumarate
Technical Data for Formoterol hemifumarate
|Storage||Store at RT|
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 Formoterol hemifumarate
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Formoterol hemifumarate
The following data is based on the product molecular weight 402.45. 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|
|0.5 mM||4.97 mL||24.85 mL||49.7 mL|
|2.5 mM||0.99 mL||4.97 mL||9.94 mL|
|5 mM||0.5 mL||2.48 mL||4.97 mL|
|25 mM||0.1 mL||0.5 mL||0.99 mL|
Product Datasheets for Formoterol hemifumarate
References for Formoterol hemifumarate
References are publications that support the biological activity of the product.
Anderson (1993) Formoterol: pharmacology, molecular basis of agonism, and mechanism of long duration of a highly potent and selective β2-adrenoceptor agonist bronchodilator. Life Sci. 52 2145 PMID: 8099696
Decker et al (1982) Effects of N-aralkyl substitution of β-agonists on α- and β-adrenoceptor subtypes: pharmacological studies and binding assays. J.Pharm.Pharmacol. 34 107 PMID: 6121868
Naline et al (1994) Relaxant effects and durations of action of formo. and salme. on the isolated human bronchus. Eur.Respir.J. 7 914 PMID: 7914176
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10 Citations for Formoterol hemifumarate
Citations are publications that use Tocris products. Selected citations for Formoterol hemifumarate include:
Bacou (2017) β2-adrenoreceptor stimulation dampens the LPS-induced M1 polarization in pig macrophages. Dev Comp Immunol 76 169 PMID: 28633932
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
Lavine et al (2013) Attenuation of choroidal neovascularization by β(2)-adrenoreceptor antagonism. JAMA Ophthalmol 131 376 PMID: 23303344
Pon et al (2016) The β2-adrenoceptor activates a positive cAMP-calcium feedforward loop to drive breast cancer cell invasion. FASEB J 30 1144 PMID: 26578688
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. Mol Cell Neurosci 11 4121 PMID: 25672589
Plummer et al (2004) Expression of inwardly rectifying potassium channels (GIRKs) and beta-adrenergic regulation of breast cancer cell lines. BMC Cancer 4 93 PMID: 15603589
McKeithan et al (2017) An Automated Platform for Assessment of Congenital and Drug-Induced Arrhythmia with hiPSC-Derived Cardiomyocytes. Front Physiol 8 766 PMID: 29075196
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
Lavine (2017) β2-Adrenergic Receptor Antagonism Attenuates CNV Through Inhibition of VEGF and IL-6 Expression. Invest Ophthalmol Vis Sci 58 299 PMID: 28114591
Koziczak-Holbro et al (2019) Pharmacological Characterization of a Novel 5-Hydroxybenzothiazolone-Derived β2-Adrenoceptor Agonist with Functional Selectivity for Anabolic Effects on Skeletal Muscle Resulting in a Wider Cardiovascular Safety Window in Preclinical Studies. J Pharmacol Exp Ther 369 188 PMID: 30819762
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Literature in this Area
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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.