Molecular Classification
G protein-coupled receptor, GPCR, Rhodopsin-like receptor
Other Names
ADRB2
Disease Roles
Beta2-Adrenergic Receptor 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.
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.
Biological Functions
Signal transduction
Smooth muscle relaxation
Bronchodilation
Regulation of intracellular cAMP levels
Disease Associations
Asthma
Chronic obstructive pulmonary disease
Conduction disorder
Preterm labour/delivery
Sleep-related breathing disorder
Obesity
Type 2 diabetes
Safety Considerations
- Tachyphylaxis (desensitization)
- Cardiovascular side effects (with some agonists)
- Genetic polymorphisms can alter drug response
Interacting Drugs
Beta2AR agonists (e.g., albuterol, salmeterol)
Epinephrine
Norepinephrine