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Human ADRB1 Reporter Assay Kit
Product Description and Product Data
This is an all-inclusive cell-based luciferase reporter assay kit targeting the the Human Adrenoreceptor Beta 1 (ADRB1). INDIGO’s ADRB1 reporter assay utilizes proprietary mammalian cells that have been engineered to provide constitutive expression of the ADRB1. In addition to ADRB1 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 ADRB1. This kit provides researchers with clear, reproducible results, exceptional cell viability post-thaw, and consistent results lot to lot. Kits must be stored at -80C. Do not store in liquid nitrogen. Note: reporter cells cannot be refrozen or maintained in extended culture.
Features
Clear, Reproducible Results
- All-Inclusive Assay Systems
- Exceptional Cell Viability Post-Thaw
- Consistent Results Lot to Lot
Product Specifications
| Target Type | GPCR | ||
| Species | Human | ||
| Receptor Form | Hybrid | ||
| Assay Mode | Agonist, Antagonist | ||
| Kit Components |
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| Shelf Life | 6 months | ||
| Shipping Requirements | Dry Ice | ||
| Storage temperature | -80C |
Data
Target Background
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 α1-, α2-, and β. Each type is further composed of three subtypes resulting in 9 different types (α1A, α1B, α1D, α2A, α2B, α2C, β1, β2, and β3).
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-1 adrenoreceptor (ADRB1) is predominantly expressed in the heart, kidney, and adipose tissue. However, their function is most often associated with the overall regulation of cardiac function. Receptor stimulation is known to be a primary control point for the modulation of heart rate and myocardial contractility. Upon binding to ligands, ADRB1 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.
Various substances, including many medications, can be used to manipulate the Beta-1 receptor. For example, Beta-blockers antagonize the binding of epinephrine and norepinephrine to the receptor thereby decreasing activity. These drugs are widely prescribed for medical conditions including hypertension, arrhythmias, migraines, and anxiety. Alternatively, Beta-agonists like isoproterenol are used to mimic and potentiate the effects of endogenous catecholamines by increasing heart rate and ventricular oxygen consumption and are commonly used in heart failure or cardiogenic shock. Consequently, the ADRB1 receptor commands considerable interest in therapeutics development and drug safety screening.
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