Protein / target
Beta-2 adrenergic receptor
Protein at a glance
Biological role
Potassium channel regulator activity
Primary system
Nervous system
Strongest disease association
stroke disorder
Therapeutic maturity
Clinically validated target
Druggability
Small molecule
Clinical development
75 approved · 17 in clinical development
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function
G protein-coupled receptor for catecholamines that couples to both G(s) and G(i) proteins, activating bifurcated signaling pathways (PubMed:2831218, PubMed:7915137). ADRB2 binds epinephrine (Epi) with an approximately 30-fold greater affinity than norepinephrine (NE) (PubMed:2831218, PubMed:33093660, PubMed:7915137). In the heart, Epi- and NE-activated ADRB2 induces rapid and slow cardiomyocyte contraction rate, respectively (By similarity). Both NE and Epi promote coupling to G(s)/PKA pathway to regulate myocyte contraction rate (By similarity). Epi also promotes ADRB2 coupling to G(i) proteins to exert cardioprotective effects especially in the conditions of hypoxia and oxidative stress through the G(i)/PI3K/Akt signaling pathway (By similarity). ADRB2-G(s) signaling delivers proapoptotic signals in cardiomyocytes although G(i)-mediated survival effect appears to predominate (By similarity). ADRB2 also transduces signals independently of PKA to regulate cellular pH by modulating Na(+)/H(+) exchanger SLC9A3 function (PubMed:9560162)
Subcellular location
Domains and Gene Ontology detail (41)Hide
Gene Ontology
- Capical plasma membrane
- Cclathrin-coated endocytic vesicle membrane
- Cendosome
- Cendosome membrane
- CGolgi apparatus
- Clysosome
- Cmembrane
- Cneuronal dense core vesicle
- Cnucleus
- Cplasma membrane
- Creceptor complex
- Fadenylate cyclase binding
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
View supporting evidenceHide supporting evidence
G protein-coupled signalling
- ·G protein-coupled receptor for catecholamines that couples to both G(s) and G(i) protein…
- ·adenylate cyclase-modulating G protein-coupled receptor signaling pathway
- ·negative regulation of G protein-coupled receptor signaling pathway
Apoptosis & cell death
- ·negative regulation of cardiac muscle cell apoptotic process
- ·positive regulation of cardiac muscle cell apoptotic process
Excitatory neurotransmission
- ·positive regulation of mini excitatory postsynaptic potential
Synaptic signalling
- ·positive regulation of mini excitatory postsynaptic potential
Proteolysis
- ·Ub-specific processing proteases
Muscle contraction
- ·regulation of smooth muscle contraction
View underlying pathways (5)Hide underlying pathways
Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Interaction neighbourhood
Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.
Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.
Drugs targeting this protein
Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.
Adrenergic receptor beta antagonist
Appears in clinical studies involving myocardial infarction, hypertensive disorder, heart failure, congestive heart failure
Adrenergic receptor agonist
Appears in clinical studies involving sudden cardiac arrest, asthma, sinusitis, septic shock
ChEMBL mechanism, action type and target identity. Open Targets clinical status and indications.
Translational evidence
Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.
Strongest genetic associations
Human genetic evidence — the most direct causal link between this target and a disease.
Highest-confidence therapeutic associations
Diseases where a drug acting on this target has already reached clinical development.
Highest overall evidence
Remaining associations by Open Targets' aggregated evidence score.
Show all associationsHide all associations
Open Targets ranks 1,315 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.
Known drugs · 96 total
hypertensive disorder · angina pectoris · myocardial infarction
asthma · Airway obstruction · renal colic
open-angle glaucoma · glaucoma
bronchial disorder
hypotensive disorder · asthma
asthma
cardiovascular disorder · migraine disorder · open-angle glaucoma
asthma · chronic obstructive pulmonary disease
chronic bronchitis · pulmonary emphysema · chronic obstructive pulmonary disease
open-angle glaucoma · glaucoma
Tractability
Safety liabilities
Clinical trials
Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein.
Show remaining trials (24)Hide
ClinicalTrials.gov via the drug-target graph.
Forefront confidence
Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.
This ranking differs from Open Targets' own: re-weighting moves genetically-evidenced diseases above more heavily co-mentioned ones. The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the underlying per-type scores are shown above so the calculation can be checked.
What's happening now
Recent activity around this target, drawn from one canonical event stream. Every item is reached through 2 drugs that target this protein, so each event is news about that drug rather than about the protein directly.
- Label change
Label change: EPINEPHRINE (NDA204640)
- Product recall
Recall (Class III): EPINEPHRINE
- Regulatory approval
Approval: Eurneffy (EMA)
- New publicationImpact of norepinephrine on immunity and oxidative metabolism in sepsis.
- New publicationMulticenter, Prospective, Randomized Controlled Trial of High-Sensitivity Cardiac Troponin I-Guided Combination Angiotensin Receptor Blockade and Beta-Blocker Therapy to Prevent Anthracycline Cardiotoxicity: The Cardiac CARE Trial.
- Label change
Label change: EPINEPHRINE (NDA204640)
- Supplemental approval
Supplemental approval: EPINEPHRINE (NDA204640)
- New publicationThe effect of topical epinephrine 1:1000 with and without infiltration of 1% lidocaine with epinephrine 1:100,000 on endoscopic surgical field visualization: a double-blind randomized controlled study.
- Indication expanded
Indication expansion: EPINEPHRINE (NDA204640)
- New publicationPulmonary arterial hypertension treatment with carvedilol for heart failure: a randomized controlled trial.
- Label change
Label change: EPINEPHRINE (NDA204640)
- Label change
Label change: EPINEPHRINE (NDA204640)
Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.