New medicine approach to reverse fentanyl overdose
Negative allosteric modulation of mu opioid receptors to reverse fentanyl overdose
This project will try compounds that change how fentanyl binds to opioid receptors so naloxone can restore breathing more quickly in people overdosing on fentanyl.
Quick facts
| Grant type | R21 grant |
|---|---|
| Study type | NIH-funded research |
| Funding institution | Trustees of Indiana University NIH-funded |
| Lab location | 1 site (Bloomington, United States) |
| Project ID | NIH-11193285 on NIH RePORTER |
What this research studies
If I'm worried about fentanyl overdose, this research is working on drugs that tweak the mu opioid receptor to make fentanyl let go or signal less strongly. The team is screening chemical relatives of cannabidiol and other negative allosteric modulators to find molecules that weaken fentanyl’s effect on the receptor. They plan lab experiments to see if these compounds speed up or strengthen naloxone’s ability to restore breathing in preclinical models. The idea is to develop a fast-acting adjunct treatment that could be given alongside naloxone in overdoses.
Who could benefit from this research
Good fit: Ideal candidates for later trials would include adults at high risk of fentanyl overdose, such as people with opioid use disorder, and healthy volunteers for early safety testing.
Not a fit: People experiencing non-opioid overdoses or those with conditions unrelated to mu opioid receptor effects would not benefit from this approach.
Why it matters
Potential benefit: If successful, this could make naloxone work faster and more reliably against fentanyl, potentially saving lives during overdoses.
How similar studies have performed: Naloxone already reverses many opioid overdoses but can fail with fentanyl, and using mu opioid receptor negative allosteric modulators is a novel approach with only preliminary laboratory evidence (for example, low-potency effects seen with CBD) and no proven human results yet.
Where this research is happening
Bloomington, United States
- Trustees of Indiana University — Bloomington, United States (Active)
Researchers
- Principal investigator: Mackie, Kenneth — Trustees of Indiana University
- Study coordinator: Mackie, Kenneth
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 below.