Target intelligence / Profile preview

Beta adrenergic receptor beta1 subtype (BETA1)

Target
BETA1
Molecular classification
GPCR, Receptor, Seven-transmembrane domain receptor
01

Overview

The beta-1 adrenergic receptor (β₁-AR), also known as ADRB1, is a member of the G protein-coupled receptor (GPCR) superfamily. It is primarily expressed in cardiac tissue but is also found in the kidney and adipose tissue. This receptor plays a central role in mediating the physiological effects of catecholamines—epinephrine and norepinephrine—on target organs, especially within the sympathetic nervous system. Activation increases heart rate, contractility, and renin release, and promotes lipolysis. Beta-blockers are drugs that antagonize BETA1 receptors and are widely used in treating hypertension, arrhythmias, and heart failure.

Other names
ADRB1
02

Mechanism of action

Beta-blockers antagonize BETA1 receptors, reducing heart rate and contractility by blocking sympathetic stimulation. Agonists like epinephrine and norepinephrine bind to BETA1, activating Gs protein, stimulating adenylyl cyclase, increasing cAMP production, and activating protein kinase A.

03

Biological functions

Signal transductionRegulation of heart rateRegulation of blood pressureLipolysis
04

Disease associations

HypertensionArrhythmiasHeart failure
05

Safety considerations

BradycardiaHypotensionBronchospasm (with non-selective beta-blockers)Fatigue
06

Interacting drugs

Metoprolol

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