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The role of adenosine receptor ligands on inflammatory pain: possible modulation of TRPV1 receptor function

Mansour Haddad1, Mohammad Alsalem2, Sara A Aldossary3

  • 1Faculty of Pharmacy, Yarmouk University, Irbid, 21163, Jordan. mansour.haddad@yu.edu.jo.

Inflammopharmacology
|December 29, 2022
PubMed

Insights

Adenosine receptors (ARs) play a role in managing inflammatory pain. Selective agonists for A1 and A3 ARs, and antagonists for A2A and A2B ARs, showed anti-nociceptive effects in rats, suggesting a new therapeutic target.

Area of Science:

  • Pharmacology
  • Neuroscience
  • Pain Research

Background:

  • Chronic pain significantly impacts health and quality of life, with current analgesics often having limited efficacy and adverse effects.
  • Adenosine receptors (ARs) are known to influence pain pathways, but the specific roles of their subtypes (A1, A2A, A2B, and A3) in pain modulation require further elucidation.

Purpose of the Study:

  • To investigate the therapeutic potential of selective adenosine receptor (AR) ligands in managing inflammatory pain.
  • To explore the anti-nociceptive effects of various AR agonists and antagonists in a rat model of inflammatory pain.

Main Methods:

  • Mechanical allodynia was induced using Complete Freund's Adjuvant (CFA) in Sprague Dawley rats.
  • The von Frey filament test was employed to assess the anti-nociceptive effects of selective AR agonists and antagonists.
  • Calcium imaging was utilized to evaluate the impact of AR ligands on capsaicin-evoked responses in dorsal root ganglia (DRG) neurons.

Main Results:

  • Selective agonists for A1AR and A3AR, along with selective antagonists for A2AAR and A2BAR, demonstrated significant anti-nociceptive effects at a dose of 1 mg/kg.
  • Co-administration of selective antagonists for A1AR and A3AR reversed the anti-nociceptive effects of their respective agonists.
  • Effective AR ligands inhibited capsaicin-evoked calcium responses in cultured DRG neurons, indicating modulation of TRPV1 activity.

Conclusions:

  • Modulation of adenosine receptors, particularly A1AR and A3AR activation and A2AAR and A2BAR blockade, shows promise for treating inflammatory pain.
  • The anti-nociceptive effects are potentially mediated through the interaction between adenosine receptors and the transient receptor potential vanilloid 1 (TRPV1) receptor.
  • Targeting the interplay between ARs and TRPV1 represents a novel therapeutic strategy for inflammatory pain conditions.
Keywords:
Adenosine receptorsInflammationPainTRPV1

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