Brain-acting medicines that target GPR88 for opioid addiction
Official title: Brain-penetrant GPR88 agonists as novel therapeutics for opioid abuse
Funded at Sanford Burnham Prebys Medical Discovery Institute · NIH-11364680 · Data updated 2026-11-12
This project develops new brain-penetrant drugs that turn on the GPR88 receptor to help reduce opioid craving, withdrawal symptoms, and addictive behaviors in people with opioid dependence.
Quick facts
| Grant type | R01 grant |
|---|---|
| Study type | NIH-funded research |
| Funding institution | Sanford Burnham Prebys Medical Discovery Institute NIH-funded |
| Lab location | 1 site (La Jolla, United States) |
| Project start | August 1, 2022 |
| Project end | July 31, 2027 |
| Funding year | 2025 |
| Award (this year) | $644,048 |
| NIH project number | 4R01DA056828-02 |
| Project ID | NIH-11364680 on NIH RePORTER |
Who could benefit from this research
✓Could help
Ideal future trial candidates would be adults with opioid use disorder who experience withdrawal or recurrent relapse despite current treatments.
✕Less likely to help
People with non-opioid substance use disorders, those seeking immediate emergency overdose care, or individuals not eligible or willing to join clinical trials are unlikely to benefit from this early-stage research.
What this research studies
From my perspective as a patient, researchers are designing small molecules that can enter the brain and activate GPR88, a receptor concentrated in brain regions involved in reward and habit. They will use high-throughput screening and medicinal chemistry to find and optimize lead compounds with properties suitable for treating opioid dependence. Leads will be tested in mouse models of opioid dependence — including genetically modified mice lacking Gpr88 — and in behavioral assays that measure withdrawal and addiction-like responses. If compounds show safety and benefit in these preclinical tests, the team plans to advance the best candidates toward clinical development.
Why it matters
Potential benefit: If successful, this work could produce a new type of medicine that lowers opioid cravings, eases withdrawal, and reduces relapse risk for people with opioid use disorder.
How similar studies have gone: Early preclinical studies in mice suggest GPR88 influences opioid signaling and show promising results, but no GPR88-targeting drugs have yet been tested in humans.
Where this research is happening
-
Sanford Burnham Prebys Medical Discovery Institute
La Jolla, United States Active
Researchers
- Principal investigator: Jackson, Michael — Sanford Burnham Prebys Medical Discovery Institute
- Study coordinator: Jackson, Michael
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About this research
- This is an active NIH-funded research project — typically early-stage science, not a clinical trial accepting patient enrollment.
- Some NIH-funded labs run parallel clinical studies or seek volunteers for related work. To check, contact the principal investigator or institution listed above.
- For full project details, budget, and progress reports, visit the official NIH RePORTER page.