Brain-acting medicines that target GPR88 for opioid addiction

Brain-penetrant GPR88 agonists as novel therapeutics for opioid abuse

['FUNDING_R01'] · SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE · NIH-11364680

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

Phase['FUNDING_R01']
Study typeNih_funding
SexAll
SponsorSANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE (nih funded)
Locations1 site (LA JOLLA, UNITED STATES)
Trial IDNIH-11364680 on ClinicalTrials.gov

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.

Who could benefit from this research

Good fit: Ideal future trial candidates would be adults with opioid use disorder who experience withdrawal or recurrent relapse despite current treatments.

Not a fit: 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.

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 performed: 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

LA JOLLA, UNITED STATES

Researchers

About this research

  1. This is an active NIH-funded research project — typically early-stage science, not a clinical trial accepting patient enrollment.
  2. Some NIH-funded labs run parallel clinical studies or seek volunteers for related work. To check, contact the principal investigator or institution listed above.
  3. For full project details, budget, and progress reports, visit the official NIH RePORTER page below.

View on NIH RePORTER →

Last reviewed 2026-05-15 by the Find a Trial editorial team. Information on this page is for educational purposes and is not medical advice. Always consult qualified healthcare professionals about clinical trial participation.