B2-Adrenergic Receptor Assay(s)

Background Information

Gs-coupled receptor mediating bronchodilation (airway smooth muscle relaxation) and cardiac stimulation. Beta-agonist inhalers (SABA and LABA) are the cornerstone of asthma and COPD treatment. Cardiac safety relevance: agonist-induced tachycardia and hypokalemia (via intracellular K⁺ shift) are key safety signals routinely screened in cardiovascular liability panels.

Family: GPCR
Protein Name: β2-adrenoceptor
Gene Name: ADRB2

Organism: Human
Therapeutic Area: Cardiovascular, Respiratory

Assay Information

Validated Assay(s): cAMP, Calcium Assay
Assay type: Cell-based
Method: Fluorescence

Instrumentation: CLARIOstar; FLIPR
Plate Format: 96- or 384-well
Expression: Transient
Cell type: HEK293; HEK293T

Testing Information

Functional Mode(s): Agonist, Antagonist
Reference compound(s): Isoproterenol

Isoproterenol concentration-response data for the human B2-adrenergic receptor in a fluorescence-based GPCR assay using HEK293 cells.
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