ADRA2A Reporter Assay System (human)

This is an all-inclusive cell-based luciferase reporter assay kit targeting the Human Adrenoceptor Alpha 2A (ADRA2A). INDIGO's ADRA2A reporter assay utilizes proprietary mammalian cells that have been engineered to provide constitutive expression of the ADRA2A. In addition to ADRA2A 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 ADRA2A. 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 Human ADRA2A Reporter Cells Cell Recovery Medium (CRM) Compound Screening Medium (CSM) Brimonidine, (ref. agonist, in DMSO) Detection Substrate Detection Buffer White, sterile, cell-culture ready assay plate. Shelf Life: 6 months. Shipping Requirements: Dry Ice. Storage temperature: -80 °C. Target Background: The adrenoceptors (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, adrenoceptor 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). Adrenoceptors 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 adrenoceptors are activated by the same endogenous catecholamines (epinephrine and norepinephrine), however, the specificity of their responses depends on the G-proteins and effector systems they associate with in a tissue and time specific manner. Adrenoceptor Alpha 2A (ADRA2A) is expressed in the central nervous system and in peripheral organs such as spleen, kidney, heart, aorta, skeletal muscle, lung and liver. ADRA2A agonists are used in general anesthesia and in the treatment of opiate withdrawal, attention deficit and hyperactive disorder (ADHD), post-traumatic stress disorder (PTSD), and Tourette's syndrome. ADRA2A also plays a role in the regulation of blood pressure, in the regulation of glucose metabolism, and in some types of cancer. Protein function: Alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p- octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol. [The UniProt Consortium]