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Protein / target

Beta-1 adrenergic receptor

Encoded byADRB1P08588Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
59
Approved medicines
Open Targets target-level
View by indication →
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Alpha-2A adrenergic receptor binding

Strongest disease association

Hypertension

Via encoding gene ADRB1 · Genetic evidence · score 0.87

Therapeutic position

Established drug target

Small molecules

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function overview

G protein-coupled receptor for catecholamines that couples to G(s) proteins to activate adenylate cyclase and cAMP-dependent pathway.

View complete UniProt function annotation

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

Cell membrane
Domains and Gene Ontology detail (18)

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

477 aa · 51 kDa

Biological roles

Reactome v97

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Synaptic signallingGOG protein-coupled signallingUniProt · GO
View supporting evidence

Synaptic signalling

  • ·Schaffer collateral - CA1 synapse
  • ·G protein-coupled neurotransmitter receptor activity involved in regulation of postsynap…

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
View underlying pathways (2)

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Interaction neighbourhood

STRING v12.0

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.

GNASARRB1ADRB2DLG4NPPAGIPPOMCGCGGNAI2GNAI1ADRB1

10 strongest partners — larger node and heavier line mean higher confidence

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.

Approved medicines with mapped indications

2 medicines · 15 areas

Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.

Angioedema1 medicine
Asthma1 medicine
Glaucoma1 medicine
Heart Arrest1 medicine
Heart Failure1 medicine
Hemorrhage1 medicine
Hypersensitivity1 medicine
Hypertension1 medicine
Lung Diseases, Obstructive1 medicine
Myocardial Infarction1 medicine
Shock, Septic1 medicine
Sinusitis1 medicine
Urticaria1 medicine
Ventricular Dysfunction, Left1 medicine
Broader indication categories (1)
Cardiovascular Diseases2 medicines

Broad umbrella indications (e.g. “Neoplasms”). Shown here because every medicine also appears under a more specific disease above — kept for completeness, de-emphasised for clarity.

59 medicines meet Open Targets' target-level approved-medicine definition; the 2 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.

Drugs targeting this protein

2

How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.

carvedilol
ApprovedAntagonist

Adrenergic receptor beta antagonist

Indicated for Heart Failure, Hypertension, Myocardial Infarction, Ventricular Dysfunction, Left

Acts on a complex — shared with ADRB2, ADRB3 · 1 of 6 recorded protein targets

Epinephrine
ApprovedAgonist

Adrenergic receptor agonist

Indicated for Angioedema, Asthma, Glaucoma, Heart Arrest

Acts on a complex — shared with ADRA1A, ADRA2A, ADRB2 +5 more · 1 of 9 recorded protein targets — broad pharmacology

ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.

Translational evidence

Open Targets 26

Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.

Strongest disease associations · via encoding gene ADRB1

Gene-level evidence surfaced through the gene ADRB1 that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.

Hypertension
0.97Well supported

Genetic evidence dominant · Open Targets 0.75

Cardiovascular Diseases
0.94Well supported

Genetic evidence dominant · Open Targets 0.71

Myocardial Infarction
0.77Well supported

Clinical evidence dominant · Open Targets 0.62

Heart Failure
0.75Well supported

Clinical evidence dominant · Open Targets 0.61

Glaucoma, Open-Angle
0.75Moderately supported

Clinical evidence dominant · Open Targets 0.61

View evidence synthesis (5)
HypertensionWell supported
0.97
agreement 0.861.00
Genetic51%Clinical44%Literature6%

Open Targets aggregate 0.75 · 3 independent evidence families

Cardiovascular DiseasesWell supported
0.94
agreement 0.831.00
Genetic51%Clinical49%Literature1%

Open Targets aggregate 0.71 · 3 independent evidence families

Myocardial InfarctionWell supported
0.77
agreement 0.610.93
Clinical89%Literature11%

Open Targets aggregate 0.62 · 2 independent evidence families

Heart FailureWell supported
0.75
agreement 0.600.91
Clinical92%Literature8%

Open Targets aggregate 0.61 · 2 independent evidence families

Glaucoma, Open-AngleModerately supported
0.75
agreement 0.590.90
Clinical99%Literature1%

Open Targets aggregate 0.61 · 2 independent evidence families

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 per-type scores above show the calculation.

Show all associations
Hypertension0.75
Cardiovascular Diseases0.71
Myocardial Infarction0.62
Heart Failure0.61
Glaucoma, Open-Angle0.61
Ocular Hypertension0.61
Glaucoma0.61
Angina Pectoris0.60
Migraine Disorders0.60

Drug development

65 compounds recorded · 59 approved · 2 in clinical development · 4 earlier-stage

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines. Distinct from the 2 drugs that target this protein in Forefront's canonical graph (2 with a mapped approved indication, shown above): these count different sets and are not a subset relation.

View all recorded compounds (10)
DROXIDOPAApproval
PROPAFENONEApproval
CARVEDILOLApproval
BETAXOLOLApproval
ESMOLOL HYDROCHLORIDEApproval
LABETALOL HYDROCHLORIDEApproval
METOPROLOL TARTRATEApproval
PENBUTOLOLApproval
BUCINDOLOLPhase 3
FOSLEVODOPAApproval

Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.

Tractability

Small moleculesStrong

Approved Drug and Structure with Ligand support this modality.

AntibodiesEmerging

Feasibility evidence (go cc high conf and uniprot loc med conf) — no clinical-stage drug of this modality recorded.

Protein degradersEmerging

Feasibility evidence (small molecule binder) — no clinical-stage drug of this modality recorded.

View underlying tractability evidence (8)
SM · Approved DrugSM · Structure with LigandSM · High-Quality LigandSM · Druggable FamilyAB · GO CC high confAB · UniProt loc med confAB · UniProt SigP or TMHMMPR · Small Molecule Binder

Raw Open Targets tractability assessment buckets, by modality.

Safety-related annotations

decreased heart rateLynch et al. (2017)increased heart rateUrban et al. (2012)electrolyte disturbancesBowes et al. (2012)increased heart rateLynch et al. (2017)relaxation of blood vesselsUrban et al. (2012)heart failureLynch et al. (2017)receptor bindingToxCastcardiovascular performanceUrban et al. (2012)decreased blood pressureBowes et al. (2012)bradycardiaUrban et al. (2012)decreased blood pressureLynch et al. (2017)edemaClinPGx

Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.

Clinical trials

30

Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.

View all trials (26)

RECRUITING · via carvedilol · NCT05931276

ClinicalTrials.gov via the drug-target graph.

What's happening now

12

Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for 2 drugs that target this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.

  1. Regulatory approval2026-09-14

    Approval: EPINEPHRINE (ANDA219832)

    fda · regulatory · fda · via Epinephrine

  2. Trial status changed2026-08-28

    Effect of Adding a Low-Dose Epinephrine Bolus Prior to Infusion on Maternal Hemodynamic Stability During Cesarean Section Under Spinal Anesthesia: A Randomized Clinical Trial

    Status changed to Completed · ClinicalTrials.gov · via Epinephrine

  3. Supplemental approval2026-08-27

    Supplemental approval: CARVEDILOL (ANDA078786)

    fda · regulatory · fda · via carvedilol

  4. Regulatory approval2026-07-31

    Approval: EPINEPHRINE (ANDA217426)

    fda · regulatory · fda · via Epinephrine

  5. Label change2026-06-22

    Label change: EPINEPHRINE (NDA204640)

    fda · regulatory · fda · via Epinephrine

  6. Product recall2026-05-14

    Recall (Class III): EPINEPHRINE

    fda · safety · fda · via Epinephrine

  7. Supplemental approval2024-10-09

    Supplemental approval: CARVEDILOL (ANDA078786)

    fda · regulatory · fda · via carvedilol

  8. Regulatory approval2024-08-22

    Approval: Eurneffy (EMA)

    ema · regulatory · ema · via Epinephrine

  9. New publication2023-11-07
    Impact of norepinephrine on immunity and oxidative metabolism in sepsis.

    Frontiers in immunology · 2023 · 33 citations · Europe PMC · via Epinephrine

  10. New publication2023-09-25
    Multicenter, 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.

    Circulation · 2023 · 53 citations · Europe PMC · via carvedilol

  11. New publication2019-10-31
    The 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.

    International forum of allergy & rhinology · 2020 · 6 citations · Europe PMC · via Epinephrine

  12. New publication1996-05-01
    The effect of carvedilol on morbidity and mortality in patients with chronic heart failure. U.S. Carvedilol Heart Failure Study Group.

    The New England journal of medicine · 1996 · 2,888 citations · Europe PMC · via carvedilol

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.