Gosset Adenosine Receptor A1 Overview
The adenosine receptor A1 (ADORA1) is a G protein-coupled receptor (GPCR) that binds adenosine. It is encoded by the ADORA1 gene located on chromosome 1q32.1. ADORA1 is ubiquitously expressed, with high expression in the central nervous system, adrenal gland, heart atrium, and smooth muscle. Upon activation by adenosine, ADORA1 inhibits adenylate cyclase, decreasing intracellular cAMP levels. It plays key roles in sleep promotion, neuroprotection, synaptic modulation, and vascular tone regulation. It is implicated in diseases such as orthostatic hypotension and Parkinson's disease. Selective agonists and antagonists have been developed as potential therapeutics.
Mechanism of Action
Gi/Go-mediated inhibition of adenylate cyclase activity, activation of phospholipase C, activation of potassium channels, inhibition of calcium channels
Biological Functions
Disease Associations
Safety Considerations
No safety concerns listed