HTS073M - ChemiScreen™ beta 2 Adrenergic Receptor Membrane Preparation

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    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 a- and β- adrenergic receptors (Bylund et al., 1994). The β-adrenergic receptors, primarily the b2 subtype, mediate relaxation of smooth muscle in many tissues, and β2-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 b-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). 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 mg/well of β2 Adrenoceptor Membrane Prep and 0.5 nM [125I]-(-)ICYP, a greater than 40-fold signal-to-background ratio was obtained.

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    Item Unit of Measure: EA
    Quantity: 200 units
    Storage: On receipt of material store at -70°C. Unopened reagent is stable for a minimum of 1 year from date of shipment when stored at recommended storage temperature. Avoid repeat freeze/thaw cycles. For maximum recovery of product, centrifuge original vial
    Applications: Radioligand Binding Assay
    Species: Full length human ADRB2 encoding β2 adrenoceptor (Accession number NM_000024).
    Host Cell: Chem-2, a suspension mammalian cell line without any endogenous β2 adrenoceptor expression.
    Reference 1: 1. Bylund DB et al. (1994). IV. International Union of Pharmacology nomenclature of adrenoceptors. Pharmacol. Rev. 46:121-136.
    Reference 2: 2. Feldman DS et al. (2005). Mechanisms of Disease: β-adrenergic receptors—alterations in signal transduction and pharmacogenomics in heart failure. Nat. Clin. Pract. Cardiovasc. Med. 2:475-83.
    Reference 3: 3. Sears MR and Lotvall J (2005). Past, present and future— β2-adrenoceptor agonists in asthma management. Respir. Med. 99:152-70.