ADRB2 Reporter Assay System (human)

This is an all-inclusive cell-based luciferase reporter assay kit targeting the the Human Adrenoreceptor Beta 2 (ADRB2). INDIGO's ADRB1 reporter assay utilizes proprietary mammalian cells that have been engineered to provide constitutive expression of the ADRB2. In addition to ADRB2 Reporter Cells, this kit provides two optimized media for use during cell culture and in diluting the user's test samples, a reference agonist, Luciferase Detection Reagent, and a cell culture-ready assay plate. The principal application of this assay is in the screening of test samples to quantify any functional activity, either agonist or antagonist, that they may exert against ADRB2. This kit provides researchers with clear, reproducible results, exceptional cell viability post-thaw, and consistent results lot to lot. Kits must be stored at -80 °C. Do not store in liquid nitrogen. Note: reporter cells cannot be refrozen or maintained in extended culture. The adrenoreceptors (a.k.a. adrenergic receptors) mediate the action of the sympathetic nervous system and are activated in response to 'fight-or-flight' signals. They are divided into three types, adrenoreceptor alpha1-, alpha2-, and beta. Each type is further composed of three subtypes resulting in 9 different types (alpha1A, alpha1B, alpha1D, alpha2A, alpha2B, alpha2C, beta1, beta2, and beta3). Adrenoreceptors belong to the G-Protein-coupled receptor (GPCR) family. They all display the characteristic seven transmembrane helices, the extracellular loops which contribute to ligand binding, and the intracellular carboxy tail that associates with trimeric G proteins. All nine types of adrenoreceptors are activated by the same endogenous catecholamines (epinephrine and norepinephrine), however, the specificity of their responses depends on the G-proteins and effectors systems they associate with in a tissue and time specific manner. The beta-2 adrenoceptor (ADRB2) is abundantly expressed in the bronchial smooth muscle cells and activation of the receptor leads to bronchodilation. In addition, ADRB2 is expressed in cardiac myocytes and vascular smooth muscle cells. Receptor stimulation is known to be a primary control point for the modulation of heart rate and myocardial contractility. Upon binding to ligands, ADRB2 undergoes a conformational change that triggers the activation of Gs proteins via an exchange of GDP with GTP, followed by the activation of adenylate cyclase and the production of the second messenger cAMP. ADRB2 is the target of clinically important drugs for asthma and cardiovascular conditions including hypertension and congestive heart failure (CHF). Various substances, including many medications, can be used to manipulate ADRB2. For example, Beta-agonists like Salbutamol and antagonists like Propranolol are among the most prescribed medications in the treatment of asthma and cardiovascular disease, respectively. Consequently, the ADRB2 receptor commands considerable interest in therapeutics development and drug safety screening. Protein function: Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately 30- fold greater affinity than it does norepinephrine. [The UniProt Consortium]