Fluorinated MU-Opioid Receptor Agonists
Summary:
Investigators at the National Institute on Drug Abuse seek co-development partners and/or licensees for collection of mu opioid receptor (MOR) agonists as alternatives for existing compounds.
Description of Technology:
Although existing opioids are excellent analgesics and useful as positron emission tomography (PET) radiotracers, they come with debilitating side effects. These include addiction, respiratory distress, hyperalgesia, and constipation. Therefore, there is a need for alternatives with lower adverse effects.
Investigators at NIDA have identified a novel fluorinated mu-opioid receptor agonist, Fluornitrazene (FNZ), a derivative of Etonitazene, that shows potent antinociceptive effects with low adverse effects. This compound does not accumulate in the brain or cause hyperalgesia. It has higher potency than morphine and fentanyl, but with fewer adverse effects. These characteristics make it and any derivatives useful as potential pain medications or anesthetics, and as therapeutics for treating opioid addiction or opioid use disorder. Compared to fentanyl, FNZ has greater potency and efficacy for the G protein activation pathway of the MOR and a lower incidence of respiratory depression in rats. This suggests that FNZ may be a better alternative to fentanyl in clinical use.
Investigators seek co-development opportunities through cooperative research and development agreement (CRADA) collaborations. This technology is also available for development under a license.
Potential Commercial Applications:
- Pain prevention or pain management
- Anesthetic
- Opioid addiction or opioid use disorder
- PET agonist radiotracer
Competitive Advantages:
- Reduced time in brain
- High potency
- MOR Selective
- No known hyperalgesia or tolerance
- Reduced side effects – such as respiratory depression