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Target intelligence / Profile preview
Beta2-Adrenergic Receptor (β₂AR)
- Target
- β₂AR
- Molecular classification
- G protein-coupled receptor, GPCR, Rhodopsin-like receptor
01
Overview
The beta2-adrenergic receptor (β₂AR), also known as ADRB2, is a G protein-coupled receptor (GPCR) primarily binding epinephrine and, to a lesser extent, norepinephrine. Activation increases intracellular cAMP, leading to smooth muscle relaxation and bronchodilation. It's a key target for asthma and COPD treatment, but polymorphisms can affect drug response.
- Other names
- ADRB2
02
Mechanism of action
Agonists bind to the β₂AR, activating adenylate cyclase via Gs proteins, leading to increased intracellular cAMP, resulting in smooth muscle relaxation and bronchodilation.
03
Biological functions
Signal transductionSmooth muscle relaxationBronchodilationRegulation of intracellular cAMP levels
04
Disease associations
AsthmaChronic obstructive pulmonary diseaseConduction disorderPreterm labour/deliverySleep-related breathing disorderObesityType 2 diabetes
05
Safety considerations
Tachyphylaxis (desensitization)Cardiovascular side effects (with some agonists)Genetic polymorphisms can alter drug response
06
Interacting drugs
Beta2AR agonists (e.g., albuterol, salmeterol)
2 more in the full profile.
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