About a quarter of patients who receive prescription opioids for long-term pain struggle with addiction, and overdose deaths involving prescription opioids have quadrupled since 1999. 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.
Recognizing that glycine receptors are responsible for the analgesic effects of marijuana. We screened a library of drug-like molecules for structural compatibility with the same glycine receptor binding site as THC. A representative compound from this group –ZINC08 –was even more effective than THC at enhancing human glycine receptor function in vitro. In mouse behavioral tests, ZINC08 reduced the effects of inflammatory pain and boosted the efficacy of a sub-therapeutic dose of morphine. Patients and prescribers could use ZINC08 and other glycine receptor modulators in its class to reduce the necessary dose of opioids for pain management. This would eliminate side effects such as dependence, tolerance, addiction, sedation, and nausea.
- Captures only the analgesic effects of THC
- Does not affect normal sensitivity to pain under non-inflammatory conditions
- Synergistic with morphine
- 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)
Stage in Development
In vitro and in vivo behavioral data
Provisional patent application filed