Adenosine A1 Receptor Antagonists

The A₁ receptor is a member of the adenosine receptor group of G-protein-coupled receptors that also includes A_2A, A_2B and A₃. A₁ receptors display high expression levels in the brain (cortex, cerebellum, hippocampus), dorsal horn of the spinal cord, eye, adrenal gland and atria. Lower expression levels are also found in the liver, kidney, skeletal muscle, adipose tissue, colon, testes, salivary glands and oesophagus. A₁ receptors play a role in lipolysis, antinociception and cardio- and neuroprotection. The human A₁ receptor gene is localized on chromosome 1 (1q32.1)