Purinergic receptors modulators: An emerging pharmacological tool for disease management

Med Res Rev. 2022 Jul;42(4):1661-1703. doi: 10.1002/med.21888. Epub 2022 May 13.

Abstract

Purinergic signaling is mediated through extracellular nucleotides (adenosine 5'-triphosphate, uridine-5'-triphosphate, adenosine diphosphate, uridine-5'-diphosphate, and adenosine) that serve as signaling molecules. In the early 1990s, purines and pyrimidine receptors were cloned and characterized drawing the attention of scientists toward this aspect of cellular signaling. This signaling pathway is comprised of four subtypes of adenosine receptors (P1), eight subtypes of G-coupled protein receptors (P2YRs), and seven subtypes of ligand-gated ionotropic receptors (P2XRs). In current studies, the pathophysiology and therapeutic potentials of these receptors have been focused on. Various ligands, modulating the functions of purinergic receptors, are in current clinical practices for the treatment of various neurodegenerative disorders and cardiovascular diseases. Moreover, several purinergic receptors ligands are in advanced phases of clinical trials as a remedy for depression, epilepsy, autism, osteoporosis, atherosclerosis, myocardial infarction, diabetes, irritable bowel syndrome, and cancers. In the present study, agonists and antagonists of purinergic receptors have been summarized that may serve as pharmacological tools for drug design and development.

Keywords: G-coupled protein receptors; adenosine; ligand-gated ion channels; purinergic signaling.

Publication types

  • Review
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine
  • Adenosine Triphosphate / metabolism
  • Disease Management
  • Humans
  • Ligands
  • Receptors, Purinergic P1* / metabolism
  • Receptors, Purinergic* / metabolism

Substances

  • Ligands
  • Receptors, Purinergic
  • Receptors, Purinergic P1
  • Adenosine Triphosphate
  • Adenosine