Brain-penetrant GPR88 agonists to help people struggling with opioid addiction
Official title: Brain-penetrant GPR88 agonists as novel therapeutics for opioid abuse
Funded at Sanford Burnham Prebys Medical Discovery Institute · NIH-11393939 · Data updated 2026-11-12
A new NIH-funded project aims to develop brain-penetrant GPR88 activating drugs to reduce opioid craving, withdrawal symptoms, and relapse risk in people with opioid use disorder.
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 | 2026 |
| Award (this year) | $581,970 |
| NIH project number | 5R01DA056828-03 |
| Project ID | NIH-11393939 on NIH RePORTER |
Who could benefit from this research
✓Could help
Ideal candidates are individuals with opioid use disorder who experience withdrawal symptoms and are seeking new treatment options.
✕Less likely to help
If a person’s opioid use disorder is not mediated by GPR88 pathways or if brain-penetrant agonists are unsuitable for their condition, benefits may be limited.
What this research studies
This project focuses on creating small-molecule drugs that can cross the blood-brain barrier and activate the GPR88 receptor in the brain. Researchers will use mouse models of opioid dependence and genetic tools to understand how GPR88 influences opioid signaling and withdrawal. The team will screen and optimize compounds to overcome previous limitations of GPR88 agonists, aiming to develop lead candidates for future development. The ultimate goal is to establish a clear path toward a therapeutic that could help people reduce opioid use and improve withdrawal management.
Why it matters
Potential benefit: If successful, this work could lead to new medications that ease withdrawal and reduce relapse risk for people with opioid use disorder.
How similar studies have gone: Preclinical studies have shown GPR88 can modulate opioid signaling, with prior agonists limited in vivo utility; this project aims to overcome those barriers.
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
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.