Protein / target
Beta-1 adrenergic receptor
Protein at a glance
Biological role
Alpha-2A adrenergic receptor binding
Primary system
Cardiovascular system
Strongest disease association
hypertensive disorder
Therapeutic maturity
Clinically validated target
Druggability
Small molecule
Clinical development
59 approved · 2 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 G(s) proteins to activate adenylate cyclase and cAMP-dependent pathway (PubMed:10212248, PubMed:12391161, PubMed:15358775). Binds epinephrine and norepinephrine with approximately equal affinity (PubMed:33093660). Mediates the activation of Ras via binding with cAMP-dependent RAPGEF2 (PubMed:12391161). As part of the sympathetic nervous system, plays a role in the physiologic regulation of cardiac functions such as stimulation of cardiomyocyte contraction (PubMed:11052857). Also delivers proapoptotic signals in cardiomyocytes (By similarity). Involved in the regulation of sleep/wake behaviors (PubMed:11854867, PubMed:31473062)
Subcellular location
Domains and Gene Ontology detail (18)Hide
Gene Ontology
- Cearly endosome
- Cneuronal dense core vesicle
- Cplasma membrane
- CSchaffer collateral - CA1 synapse
- Falpha-2A adrenergic receptor binding
- Fbeta-adrenergic receptor activity
- Fbeta1-adrenergic receptor activity
- FG protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic membrane potential
- FPDZ domain binding
- Fprotein heterodimerization activity
- Padenylate cyclase-activating adrenergic receptor signaling pathway
- Padenylate cyclase-activating G protein-coupled receptor signaling pathway
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 G(s) proteins to activate…
- ·G protein-coupled neurotransmitter receptor activity involved in regulation of postsynap…
- ·adenylate cyclase-activating G protein-coupled receptor signaling pathway
Synaptic signalling
- ·Schaffer collateral - CA1 synapse
- ·G protein-coupled neurotransmitter receptor activity involved in regulation of postsynap…
Apoptosis & cell death
- ·positive regulation of cardiac muscle cell apoptotic process
View underlying pathways (2)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 601 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 · 65 total
orthostatic hypotension · multiple system atrophy · cardiovascular disorder
cardiac arrhythmia · ventricular fibrillation · atrial fibrillation
myocardial infarction · hypertensive disorder · heart failure
cardiovascular disorder · Hypertension · glaucoma
hypertensive disorder · diabetic foot · Tachycardia
hypertensive disorder
myocardial infarction · hypertensive disorder · angina pectoris
cardiovascular disorder · Hypertension
heart failure · atrial fibrillation · Hypertension
Parkinson disease · Parkinson disease · Parkinson disease
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.
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.