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Target intelligence / Profile preview
Adenosine Receptor A1 (A1AR)
- Target
- A1AR
- Molecular classification
- G protein-coupled receptor, GPCR, Receptor
01
Overview
The adenosine A1 receptor (A1AR) is a G protein-coupled receptor that binds adenosine. It is widely distributed throughout the body, particularly in the brain, heart, and kidneys, and plays a crucial role in regulating various physiological functions, including sleep, neuronal activity, cardiac function, and renal blood flow. Activation of A1AR primarily inhibits adenylyl cyclase, leading to decreased cAMP levels, and modulates ion channels, resulting in inhibitory effects. As such, it is a drug target for cardiac arrhythmias, neuroprotection, and pain management.
- Other names
- A1 receptorADORA1
02
Mechanism of action
Activation of Gi/o proteins leading to decreased cAMP levels, activation of potassium channels, and inhibition of calcium channels.
03
Biological functions
Signal transductionNeuromodulationCardiac function regulationRenal function regulationInhibition of neurotransmitter releaseSleep promotion
04
Disease associations
Cardiac arrhythmiasNeurodegenerative diseasePainIschemic eventsStrokeSleep disorders
05
Safety considerations
Non-selective targeting may lead to off-target effects.Systemic hypotension with adenosine agonists.Potential for drug interactions due to widespread tissue distribution.
06
Interacting drugs
Adenosine
3 more in the full profile.
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