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Target intelligence / Profile preview
Beta-2 adrenergic receptor (ADRB2)
- Target
- ADRB2
- Molecular classification
- GPCR, G protein-coupled receptor, Rhodopsin family, Receptor
01
Overview
The beta-2 adrenergic receptor (β2AR), also known as ADRB2, is a G protein-coupled receptor (GPCR) located on the cell membrane. It primarily binds epinephrine (adrenaline), with about 30-fold higher affinity than norepinephrine. This interaction triggers intracellular signaling cascades that mediate physiological responses such as smooth muscle relaxation and bronchodilation. Polymorphisms in this gene are associated with conditions like nocturnal asthma, obesity, and type 2 diabetes. It is a major target for inhaled agonists in asthma and COPD therapy.
- Other names
- β2ARADRB2
02
Mechanism of action
Agonist binding activates Gs proteins, stimulating adenylate cyclase, increasing intracellular cAMP levels, leading to downstream effects such as L-type calcium channel modulation and smooth muscle relaxation.
03
Biological functions
Smooth muscle relaxationBronchodilationMetabolic regulationSignal transduction
04
Disease associations
AsthmaChronic obstructive pulmonary disease (COPD)Conduction disordersPreterm labor/deliverySleep-related breathing disordersObesityType 2 diabetes
05
Safety considerations
Cross-reactivity with other adrenoceptorsPotential for adverse effects depending on drug selectivity and patient-specific factors
06
Interacting drugs
Albuterol
5 more in the full profile.
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