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NEW COMPOUNDS FOR THE TREATMENT OF ACUTE PAIN

Acute pain management; Antinociceptive activity;

Introduction

The invention refers to new compounds for the treatment of acute pain. Current therapeutic approaches to pain management include the use of opioids which showed many side effects, including tolerance and potential dependency. The present invention allows the development of new therapeutic strategies and new non-opioid drugs for the pain management.

Technical features

The invention describes the development of new compounds of thiazole [5,4-d] pyrimidine structure which are more powerful adenosine A2A receptor blockers than those already present on the market. Affinity and potency of the compounds were evaluated by receptor binding experiments and cyclic AMP assays. From these tests it is clear that the new compounds have a high affinity (femtomolar order) for the A2A receptor, associated with a high power (picomolar order). In addition, the new derivatives were tested in animal models of acute pain, widely used and validated, such as writhing and tail immersion tests, and were effective similar or superior to morphine.

Possible Applications

  • Treatment of acute pain;
  • Inflammation;
  • Fibrosis;
  • Cancer;
  • Neurodegenerative diseases.

Advantages

  • Two compounds (13 and 14) in functional tests of cyclic AMP, showed a potency of the picomolar order, higher than that of A2A receptor blockers already commercially available (1);
  • The new compounds (13 and 14) showed an antinociceptive effect equal to or greater than morphine and the reference compound (1) in writhing and in the tail immersion test.