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Target intelligence / Profile preview
Beta 1-Adrenergic Receptor (ADRB1)
- Target
- ADRB1
- Molecular classification
- G-protein-coupled receptor (GPCR), Class A GPCR, Receptor
01
Overview
The beta 1 adrenergic receptor is a critical regulator of cardiovascular physiology through its role as a GPCR responsive to catecholamines. Its predominant expression on cardiomyocytes underlies its central role in modulating cardiac output via chronotropic/inotropic mechanisms while serving additional functions in renal renin secretion and adipocyte metabolism. Its pharmacological importance makes it one of the most studied targets for cardiovascular therapeutics.
- Other names
- β1-adrenergic receptorADRB1 receptorBeta-1 Adrenoceptorβ1-AR
02
Mechanism of action
Gs protein activation, adenylyl cyclase activation, increased cAMP production, protein kinase A (PKA) activation, downstream phosphorylation events leading to increased heart rate, contractility, and renin release.
03
Biological functions
Signal transductionRegulation of heart rateRegulation of cardiac contractilityRenin secretionLipolysisRegulation of atrioventricular node conduction
04
Disease associations
HypertensionArrhythmiaAngina pectorisHeart failureCardiovascular disease
05
Safety considerations
BradycardiaHypotensionAV blockHeart failure exacerbationMasking of hypoglycemia symptoms in diabetic patientsBronchoconstriction (less common with selective β1-blockers but possible in susceptible individuals)
06
Interacting drugs
Epinephrine
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