Target intelligence / Profile preview

Adrenergic receptor (AR) (AR)

Target
AR
Molecular classification
G-protein-coupled receptor, Rhodopsin-like GPCR, 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. They are broadly categorized into alpha and beta types, which are further divided into nine distinct subtypes that exhibit unique tissue distributions and signaling mechanisms [1][2]. These receptors play a critical role in the sympathetic nervous system, regulating the "fight-or-flight" response by influencing heart rate, blood pressure, and airway diameter. Alpha receptors primarily mediate vasoconstriction and smooth muscle contraction, while beta receptors are involved in increasing cardiac output and inducing bronchodilation [1][3]. Because of their widespread influence on vital organ systems, adrenergic receptors are major therapeutic targets for conditions such as hypertension, heart failure, asthma, and allergic reactions. Drugs targeting these receptors include both agonists, which activate the receptors to treat conditions like shock or asthma, and antagonists, which block them to manage cardiovascular diseases [2][4].

Other names
AdrenoceptorAdrenoreceptorCatecholamine receptorAlpha and beta adrenoceptors
02

Mechanism of action

Adrenergic receptors function as G-protein-coupled receptors that respond to endogenous catecholamines. Alpha-1 receptors couple to Gq proteins to increase intracellular calcium; Alpha-2 receptors couple to Gi proteins to inhibit adenylate cyclase and decrease cAMP; and Beta receptors (1, 2, and 3) couple to Gs proteins to stimulate adenylate cyclase and increase cAMP levels [1][2].

03

Biological functions

Signal transductionSympathetic nervous system regulationSmooth muscle contractionSmooth muscle relaxationHeart rate regulationMetabolism
04

Disease associations

HypertensionHeart failureAsthmaGlaucomaAnaphylaxisBenign prostatic hyperplasia
05

Safety considerations

Bronchospasm in susceptible patients (e.g., asthma, COPD)Orthostatic hypotensionBradycardiaMasking of hypoglycemic symptoms in diabetic patientsRebound hypertension upon sudden withdrawal
06

Interacting drugs

Epinephrine

9 more in the full profile.

07

Biomarkers

Heart rateBlood pressureForced expiratory volume in 1 second (FEV1)Plasma catecholamine levels

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