Novel Glycine Receptor Modulators for Analgesia

ZINC08 is even more effective than THC at enhancing human glycine receptor function in vitro and reduced the effects of inflammatory pain and boosted the efficacy of a sub-therapeutic does of morphine.  

ZINC08, a representative of our new class of glycine receptor modulators, is more effective than THC at enhancing the function of human glycine receptors.

Description

About a quarter of patients who receive prescription opioids for long-term pain struggle with subsequent addiction, and overdose deaths. THC, the main chemical component of marijuana, has gained popularity as an alternative analgesic for treating chronic pain, but psychoactive side effects and political controversy have stymied widespread adoption. Our new class of compounds avoids these issues by capturing only the pain relief aspect of THC, potentially reducing the need for opioids.

Applications

• Treating hypersensitivity to inflammatory pain
• Treating pain from surgery, tissue damage, infection, neuropathic conditions, or skeletal muscular conditions
• Reducing the necessary dose of opioids for chronic pain management
• Prophylactic pain relief (e.g., to prevent surgical pain or anticipated opioid withdrawal pain)

Advantages

• Its effects are similar to analgesic properties of THC, without the psychoactive side effects and cultural stigma
• Does not affect normal sensitivity to pain under non-inflammatory conditions
• Synergistic with morphine, allowing sub-therapeutic doses to be effective

Invention Readiness

In vitro and in vivo behavioral data

IP Status

https://patents.google.com/patent/US20200215047A1 https://patents.google.com/patent/WO2019018241A1

Related Publication(s)

Wells, M. M., Tillman, T. S., Mowrey, D. D., Sun, T., Xu, Y., & Tang, P. (2015). Ensemble-Based Virtual Screening for Cannabinoid-Like Potentiators of the Human Glycine Receptor α1 for the Treatment of Pain. Journal of Medicinal Chemistry, 58(7), 2958–2966. https://doi.org/10.1021/jm501873p