Molecular Classification
G protein-coupled receptor, GPCR, Receptor
Other Names
Beta-adrenergic receptor, β-AR, ADRB, Beta receptor
Disease Roles
HypertensionArrhythmiasAngina pectoris

Beta-Adrenoreceptor Overview

Beta-adrenoreceptors (β-adrenoceptors) are a class of G protein-coupled receptors (GPCRs) that mediate the physiological effects of catecholamines, primarily norepinephrine and epinephrine. They play critical roles in regulating cardiovascular, respiratory, metabolic, and central nervous system functions. There are three main subtypes: β1, β2, and β3, each with distinct tissue distributions and physiological roles. Activation leads to increased cAMP production and downstream signaling. Ligands include endogenous catecholamines and synthetic agonists/antagonists. Beta-blockers are widely used for treating cardiovascular conditions and anxiety, while beta agonists serve as bronchodilators.

Mechanism of Action

Agonist binding leads to stimulation of adenylyl cyclase, increasing intracellular cAMP, activating PKA, and leading to diverse cellular responses. Antagonists block the receptor, preventing activation by endogenous ligands.

Biological Functions

Signal transduction
Regulation of heart rate
Regulation of smooth muscle tone
Regulation of metabolism
Neurotransmission

Disease Associations

Hypertension
Arrhythmias
Angina pectoris
Heart failure
Asthma
COPD
Anxiety disorders

Safety Considerations

  • Beta-blockers can cause bradycardia, hypotension, and bronchospasm.
  • Beta-agonists can cause tachycardia, tremors, and anxiety.

Interacting Drugs

Norepinephrine
Epinephrine
Isoproterenol
Propranolol