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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.
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.
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