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Biaryl amides or ureas as TRPV1 ligands

FAAH inhibitorsPain therapyPET imaging radiotracersTRPV1 ligands

Introduction

The invention relates to high affinity compounds, able to bind the transient receptor potential cation channel, subfamily Vanilloid type 1 (TRPV1), and to inhibit the Fatty Acid Amide Hydrolase (FAAH). These compounds find application in pain therapy and as novel radiotracers for Positron Emission Tomography (PET) imaging.

Technical features

Being both the receptor and the enzyme involved in pain processing and neurogenic inflammatory responses, the compounds find application in medical conditions involving the endovanilloid and endocannabinoid systems, in particular as agents for pain, anti-inflammatory, cluster headache, anti-oxidant and anti-cancer therapy. TRPV1 agonists are expected to be more powerful analgesic drugs than TRPV1 antagonists as they simultaneously block all receptors on capsaicin-sensitive nerves. Dual TRPV1 agonist/FAAH blocker compounds may offer the unusual possibility to target simultaneously two pathways relevant for the same disease, while not causing addiction and tachyphylaxis. Moreover, the chemical structure of these compounds provides the opportunity of developing new radiotracers for PET imaging. These radiotracers are of great relevance for mapping TRPV1 receptors in pathological conditions.

Possible Applications

  • Pharmacological tools for studying endovanilloid and endocannabinoid related physiopathological conditions;
  • Radiotracers for Positron Emission Tomography (PET) imaging.

Advantages

  • Simple and fast synthesis;
  • Generation of a library of compounds;
  • High selectivity against TRPv1 receptor or dual TRPV1 agonist/FAAH blocker activity;
  • Powerful analgesic drugs;
  • No central drawbacks (not addictive or toxic, stable).