Target intelligence / Profile preview

Adrenergic receptor (ADR) (ADR)

Target
ADR
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

Adrenergic receptors, also known as adrenoceptors, are a class of G protein-coupled receptors that mediate the physiological responses to the catecholamines epinephrine and norepinephrine [2, 5, 8]. They are integral components of the sympathetic nervous system, categorized into alpha (alpha-1, alpha-2) and beta (beta-1, beta-2, beta-3) subtypes based on their pharmacological profiles and signaling pathways [1, 8, 12]. Epinephrine serves as a primary endogenous ligand, acting as a non-selective agonist that triggers diverse effects such as increased heart rate, bronchodilation, and peripheral vasoconstriction [3, 6, 10]. These receptors are critical therapeutic targets; agonists like epinephrine are life-saving in anaphylaxis and cardiac arrest, while antagonists (beta-blockers and alpha-blockers) are widely used to manage hypertension and chronic heart failure [1, 8]. Understanding the subtype-specific distribution and signaling is essential for developing selective drugs that minimize off-target effects [12].

Other names
AdrenoceptorEpinephrine receptorAdrenaline receptor
02

Mechanism of action

Agonism or antagonism of alpha and beta-adrenergic receptors to modulate sympathetic nervous system activity, affecting smooth muscle contraction, heart rate, and metabolic rate.

03

Biological functions

Signal transductionSympathetic nervous system regulationVasoconstrictionVasodilationBronchodilationHeart rate regulationMetabolism
04

Disease associations

Cardiovascular diseaseAsthmaAnaphylaxisGlaucomaShockHypertension
05

Safety considerations

TachycardiaArrhythmiaHypertensionMyocardial ischemiaHyperglycemiaHypokalemiaAnxietyTremor
06

Interacting drugs

Epinephrine

11 more in the full profile.

07

Biomarkers

Heart rateBlood pressurePlasma catecholamine levelsForced expiratory volume (FEV1)

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