HUMAN RECOMBINANT α2B RECEPTOR
MULTISCREEN™ STABLE CELL LINES
1 vial (2 x 106) frozen cells
Sigma Freezing Medium (C- 6164)
Expression vector containing full-length human ADRA2B cDNA (GenBank Accession Number NM_000682.5) with FLAG tag sequence at N-terminus
Liquid nitrogen upon receiving
Propagation Medium: DMEM/F12, 10% FBS, 10 μg/mL puromycin
Stable in culture for minimum of two months
Background: Adrenergic α2b receptor belongs to the group of nine adrenoceptors that mediate the biological actions of the endogenous catecholamines adrenaline and noradrenaline. While α2a receptor exerts a tonic sympathoinhibitory function, the α2b is responsible for the central hypertensive sympathoexcitatory response. Development of agents capable of selectively activating the α2a or blocking the α2b may further improve our capability to treat hypertension, ischemic heart disease and heart failure. The α2b receptor also contributes to the peripheral regulation of vascular tone.
Application: Functional assays
Figure 1. Dose-dependent stimulation of calcium flux upon treatment with ligand, measured with MULTISCREENTM Calcium 1.0 No Wash Assay Kit (Multispan MSCA01). Figure 2. Dose-dependent increase of intracellular cAMP level upon treatment with ligand, measured with MULTISCREENTM TR-FRET cAMP 1.0 No Wash Assay Kit (Multispan MSCM01). Cells were pre-treated with pertussis toxin. Figure 3. Dose-dependent inhibition of forskolin- stimulated intracellular cAMP level upon treatment with ligand, measured with MULTISCREENTM TR-FRET cAMP 1.0 No Wash Assay Kit (Multispan MSCM01). Cells were not pre-treated. Figure 4. Receptor expression on cell surface measured by flow cytometry (FACS) using an anti-FLAG antibody. Thin line: parental cells; thick line: receptor-expressing cells.
Knaus et al (2007) Alpha2-adrenoceptor subtypes–unexpected functions for receptors and ligands derived from gene-targeted mouse models. Neurochem Int 51:277-281.
Philipp et al. (2002) Physiological significance of alpha(2)-adrenergic receptor subtype diversity: one receptor is not enough. Am J Physiol Regul Integr Comp Physiol. 283:R287-R295.