Target intelligence / Profile preview

Adenosine A1 Receptor (A1AR)

Target
A1AR
Molecular classification
G protein-coupled receptor
01

Overview

The adenosine A1 receptor (A1AR) is a G protein-coupled receptor that binds adenosine. It is widely expressed, particularly in the central nervous system and cardiovascular system, where it mediates a variety of physiological effects including neuromodulation, cardioprotection, and regulation of sleep. A1AR activation generally has an inhibitory effect on cellular activity. Dysregulation of A1AR is implicated in various diseases, and selective ligands are under development for therapeutic applications.

Other names
RDC7adenosine receptor A1A1RA₁R
02

Mechanism of action

Agonists: Activation of Gi/o proteins, inhibition of adenylate cyclase, activation of potassium channels, inhibition of calcium channels. Antagonists: Blockade of adenosine binding and downstream signaling.

03

Biological functions

Signal transductionNeuromodulationNeuroprotectionCardioprotectionRegulation of heart rateRegulation of vascular tensionInhibition of neurotransmitter releaseSleep promotion
04

Disease associations

Cardiovascular diseaseNeurodegenerative diseaseSleep disordersPainIschemia-reperfusion injury
05

Safety considerations

Potential cardiovascular effects (bradycardia, hypotension)CNS effects (sedation, dizziness)Off-target effects due to adenosine's widespread actions

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