About Adenosine

Adenosine

Ubiquitous & important molecule that is a building block of life. Adenosine acts in the body by binding to and activating four receptor subtypes (A1R, A2AR, A2BR, and A3R) found in varying density in numerous tissues throughout the body.

Adenosine is usually the product of the hydrolysis of extracellular adenosine triphosphate (ATP) and is widely distributed in the human body. It causes or modulates a variety of functions, including cell growth, heart rhythm, immune function, sleep regulation, and angiogenesis. Adenosine acts by activating specific G protein-coupled receptors (GPCRs), which are divided into four subtypes: the adenosine 1 receptor (A1R), adenosine 2A receptor (A2AR), adenosine 2B receptor (A2BR), and adenosine 3 receptor (A3R). Extensive investigations over the past 40 years have identified numerous effects of the adenosine receptors as shown below, identifying them as potential drug targets for treating numerous diseases.

A1 Receptor Effects

Cardiac

  • Negative inonotrobic
  • Negative chornotrophic

Brain

  • Reduced neuronal excitation
  • Sleep induction
  • Reduce seizures

Adipose Tissue (fat)

  • Antilipolytic

A2A Receptor Effects

Blood Vessels

  • Vasodilatation

Brain

  • Regulation of locomotion
  • Sleep

Blood Cells

  • Reduced cytokine release 
  • Reduced T-cell activation 
  • Reduced platelet activation 

A2B Receptor Effects

Cancer: Myloid/ Dendritic Cells

  • Reduced antigen presentation
  • Reduced IL-12

Cancer: Tumors

  • Reduced cell adhesion

Endothelial/Epithelial cells, Fibroblasts 

  • Enhanced IL-6 release

Adipose tissue (fat) 

  • Enhanced lipolysis

Mast cells

  • Degranulation (primates) 

Other

  • Pain enhancement (allodynia)

A3 Receptor Effects

Degranulation

  • Mast cells/Basophils (rodents)
  • White blood cells (Eosinophils)

Brain

  • Reduced neuropathic pain

Testis

  • Sperm motility

Adovate’s chemistry platform, combined with its pharmacology and development experience, is poised to harness these effects with new, potent and selective drugs that achieve biodistribution by developing antagonists (blockers) or agonists (activators) to solicit the desired response(s) while avoiding the undesired side effects characteristic of activity on the other receptors.