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48-602MAG
Buffer Detection Kit for Magnetic Beads
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HTS073M
Sigma-AldrichChemiScreen™ Recombinant Human β2 Adrenoceptor
Human beta 2 GPCR membrane preparation for Radioligand binding Assays & GTPγS binding.
The endogenous catecholamines epinephrine and norepinephrine have profound effects on smooth muscle activity, cardiac function, carbohydrate and fat metabolism, hormone secretion, neurotransmitter release, and central nervous system actions. These activities are mediated by GPCRs belonging to two subfamilies, the α- and β -adrenergic receptors (Bylund et al., 1994). The β -adrenergic receptors, primarily the β2 subtype, mediate relaxation of smooth muscle in many tissues, and β 2-selective agonists are the preferred drugs for stimulating bronchodilation in the treatment of asthma and chronic obstructive pulmonary disease (Sears and Lotvall, 2005). Activation of the β-adrenergic receptors, primarily the β1 subtype and to a lesser extent the β2 subtype, acutely increases heart rate, cardiac output, and cardiac automaticity, and chronically increases cardiac myocyte apoptosis. As a result, β -adrenergic receptor antagonists (β blockers) are effective in the treatment of congestive heart failure and arrhythmia (Feldman et al., 2005). Chemicon's β2 adrenoceptor membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high-level of GPCR surface expression; thus, they are ideal HTS tools for screening of antagonists of β2 adrenoceptor interactions with (-)Iodocyanopindolol (ICYP). The membrane preparations exhibit a Kd of 0.51 nM for [125I]-(-)ICYP. With 5 µg/well β2 Adrenoceptor Membrane Prep and 0.5 nM [125I]-(-)ICYP, a greater than 40-fold signal-to-background ratio was obtained.
References
Product Information
Format
Membranes
Presentation
One package contains enough membranes for at least 200 assays (units), where an unit is the amount of membrane that will yield greater than 40-fold signal:background with 125I-labeled (-)Iodocyanopindolol at 0.5 nM. Liquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA with no preservatives. Packaging method: Membranes protein were adjusted to the indicated concentration in packaging buffer, rapidly frozen, and stored at -80oC.
The beta-adrenergic receptor kinase specifically phosphorylates the agonist-occupied form of the beta-adrenergic and related G protein-coupled receptors. Overall, the beta adrenergic receptor kinase 2 has 85% amino acid similarity with beta adrenergic receptor kinase 1, with the protein kinase catalytic domain having 95% similarity. These data suggest the existence of a family of receptor kinases which may serve broadly to regulate receptor function.
FUNCTION: SwissProt: P35626 # Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors. SIZE: 688 amino acids; 79710 Da SIMILARITY: SwissProt: P35626 ## Belongs to the protein kinase superfamily. AGC Ser/Thr protein kinase family. GPRK subfamily. & Contains 1 AGC-kinase C-terminal domain. & Contains 1 PH domain. & Contains 1 protein kinase domain. & Contains 1 RGS domain.
Incubation Conditions
Membranes are mixed with radioactive ligand and unlabeled competitor (see Figures 1 and 2 for concentrations tested) in binding buffer in a nonbinding 96-well plate, and incubated for 1-2 h. Prior to filtration, a GF/C 96-well filter plate is coated with 0.33% polyethyleneimine for 30 min, then washed with 50mM HEPES, pH 7.4. Binding reaction is transferred to the filter plate, and washed 3 times (1 mL per well per wash) with Wash Buffer. The plate is dried and counted.
Binding buffer: 50 mM Hepes, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, filtered and stored at 4°C Radioligand: [125I]-(-) Iodocyanopindolol (Perkin Elmer # NEX189) Wash Buffer: 50 mM Hepes, pH 7.4, 500 mM NaCl, filtered and stored at 4°C.
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Signal:background and specific binding values obtained in a competition binding assay with varying amounts of β2 adrenoceptor membrane prep.
Unless otherwise stated in our catalog or other company documentation accompanying the product(s), our products are intended for research use only and are not to be used for any other purpose, which includes but is not limited to, unauthorized commercial uses, in vitro diagnostic uses, ex vivo or in vivo therapeutic uses or any type of consumption or application to humans or animals.
Storage and Shipping Information
Storage Conditions
Maintain frozen at -70°C for up to 2 years. Do not freeze and thaw.
Packaging Information
Material Size
200 units
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Bestellnummer
GTIN
HTS073M
04053252369414
Documentation
ChemiScreen™ Recombinant Human β2 Adrenoceptor SDB
Past, present and future--beta2-adrenoceptor agonists in asthma management. Sears, Malcolm R and Lötvall, Jan Respiratory medicine, 99: 152-70 (2005)
2004
The beta-adrenoceptor agonists (beta-agonists) have been used to relieve bronchoconstriction for at least 5000 years. beta-agonists are based on adrenaline and early forms, such as isoprenaline, Lacked bronchial selectivity and had unpleasant side effects. Modern beta-agonists are more selective for the beta2-adrenoceptors (beta2-receptors) located in bronchial smooth muscle and have less cardiotoxicity. Traditional beta2-adrenoceptor agonists (beta2-agonists), such as salbutamol, terbutaline and fenoterol, were characterised by a rapid onset but relatively short duration of action. While valuable as reliever medication, their short duration gave inadequate night-time relief and limited protection from exercise-induced bronchoconstriction. beta2-agonists with longer durations of action, formoterol and salmeterol, were subsequently discovered or developed. When combined with inhaled corticosteroids they improved lung function, and reduced symptoms and exacerbations more than an increased dose of corticosteroids. However, tolerance to the bronchprotective effects of long-acting beta2-agonists and cross-tolerance to the bronchodilator effects of short-acting beta2-agonists is apparent despite use of inhaled corticosteroids. The role of beta2-receptor polymorphisms in the development of tolerance has yet to be fully determined. Formoterol is unique in having both a long-lasting bronchodilator effect (> 12 h) and a fast onset of action (1-3min from inhalation), making it effective both as maintenance and reliever medication. The recent change in classification from short- and long-acting beta2-agonists to rapid-acting and/or long-acting agents reflects the ongoing evolution of beta2-agonist therapy.
Mechanisms of disease: beta-adrenergic receptors--alterations in signal transduction and pharmacogenomics in heart failure. Feldman, David S, et al. Nature clinical practice. Cardiovascular medicine, 2: 475-83 (2005)
2004
Beta-adrenergic signaling is an important regulator of myocardial function. During the progression of heart failure (HF), a reproducible series of biochemical events occurs that affects beta-adrenergic receptor (beta-AR) signaling and cardiac function. Furthermore, there are pathophysiologic alterations in the expression and regulation of proteins that are regulated by beta-ARs during HF. Analyses of these complex signaling pathways have led to a better understanding of HF mechanisms and the use of beta-adrenergic antagonists, which have notably altered HF-related morbidity and mortality. Despite therapeutic advances that have affected beta-AR signaling, HF remains a leading cause of hospitalization and a principal cause of death in industrialized nations. In this review, we summarize current insights into beta-adrenergic signal-transduction pathways, the best-described beta-AR polymorphisms, and therapies that target the beta-AR pathway in HF.
Millipore offers a large selection of robust and reliable G-protein coupled receptor products, including Stable Cell Lines, Membrane Preparations, and Frozen Cells. See below for GPCR research tools. Weitere Informationen >>
