Endacea, Inc. - Science

Adenosine-Based Technologies

Adenosine receptors are extracellular proteins located on a number of different cell types in the human body. They are coupled to intracellular signaling pathways and activation of these receptors produces a number of different physiological and pathophysiological effects. Four human adenosine receptors (ARs) have been cloned: A1, A2a, A2b, and A3. Activation of these ARs produces the following effects:

  • A1 ARs: slowing of heart, depression of heart contractility, bronchoconstriction, renal and pulmonary vasoconstriction, proinflammatory cellular effects, angiogenesis, sleep induction, and antinociception.
  • A2a ARs: vasodilation, inhibition of platelet aggregation, pain at peripheral sites, and anti-inflammatory cellular effects.
  • A2b ARs: hydration of the airway; release of cytokines from human airway bronchial and smooth muscle cells and fibroblasts; anti-inflammatory cellular and bronchorelaxant effects; decrease endothelial permeability.
  • A3 ARs: anti-inflammatory cellular effects.

For a thorough and up to date review of ARs, see Wilson CN, Mustafa SJ (eds.), Adenosine Receptors in Health and Disease, Handbook of Experimental Pharmacology 193, Springer-Verlag Berlin Heidelberg 2009.