Target intelligence / Profile preview

Cardiac cell-surface receptor

Molecular classification
Receptor, G protein-coupled receptor, Ion channel, Enzyme-linked receptor
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Overview

The term 'Cardiac cell-surface receptor' refers to a broad and heterogeneous group of proteins located on the plasma membrane of cardiomyocytes and other cardiac cells (StatPearls, 2023). These receptors, which include G protein-coupled receptors (GPCRs) like beta-adrenergic and muscarinic receptors, as well as ion channels and growth factor receptors, are essential for regulating heart rate, contractility, and electrical signaling (British Journal of Pharmacology, 2018). Because this term describes a functional class rather than a specific molecular entity, it is not considered a single therapeutic target (Nature Reviews Drug Discovery, 2020). Instead, specific members of this class are targeted by a wide range of cardiovascular drugs, such as beta-blockers and angiotensin II receptor blockers, to treat conditions like hypertension, heart failure, and arrhythmias (Circulation Research, 2019). Accurate drug development requires identifying the specific receptor subtype involved in a disease process to ensure efficacy and minimize off-target effects (Journal of the American College of Cardiology, 2021).

Other names
Myocardial cell-surface receptorHeart cell-surface receptorCardiomyocyte surface receptor
02

Mechanism of action

The mechanism of action varies significantly depending on the specific receptor subtype; for instance, beta-adrenergic antagonists (beta-blockers) inhibit sympathetic stimulation to reduce heart rate and contractility, while angiotensin II receptor blockers (ARBs) prevent vasoconstriction and fluid retention by blocking the AT1 receptor (StatPearls, 2023; Circulation Research, 2019).

03

Biological functions

Signal transductionRegulation of heart rateRegulation of myocardial contractilityElectrophysiological signalingCardiac remodeling
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Disease associations

Cardiovascular diseaseHeart failureArrhythmiaHypertensionMyocardial infarction
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Safety considerations

BradycardiaHypotensionElectrolyte imbalancesPro-arrhythmic effectsOff-target systemic effects
06

Interacting drugs

Metoprolol

5 more in the full profile.

07

Biomarkers

N-terminal pro-b-type natriuretic peptide (NT-proBNP)Cardiac troponin ICardiac troponin TSoluble ST2

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