# Buprenorphine analogs for the treatment of opioid abuse

> **NIH NIH R01** · WAKE FOREST UNIVERSITY HEALTH SCIENCES · 2022 · $697,628

## Abstract

PROJECT SUMMARY
The recent marked increase in misuse and abuse of opioids and the epidemic of opioid overdose mortality
have greatly affected our society. Given that non-human primate models offer the most phylogenetically
appropriate evaluation of opioid receptor functions and drug effects, the goal of this proposal is to establish a
translational bridge for the functional profiles of buprenorphine analogs to ameliorate opioid-assoicated side
effects in primates. Previous studies demonstrate that a buprenorphine analog BU08028 with mixed mu opioid
peptide (MOP) and nociceptin/orphanin FQ peptide (NOP) partial agonist activities is a safe analgesic without
abuse liablity. The proposal will further investigate the funcitional profiles of buprenorphine-inspired
compounds, BU08028 and BU14003, in modulating three major aspects of opioid use disorder, i.e., abuse
liability, relapse, and physical dependence. The proposal contains three aims: 1) To distinguish the functional
profiles of buprenorphine-inspired compounds from opioids following acute and chronic administration. 2) To
demonstrate the functional effectiveness of buprenorphine-inspired compounds to attenuate the abuse-related
effects of opioids including oxycodone and heroin. 3) To demonstrate the functional effectiveness of
buprenorphine-inspired compounds to alleviate the adverse effects from opioid dependence. These non-
human primate behavioral assays have been designed specifically to reflect the therapeutic potential of
buprenorphine-inspired compounds for inhibiting opioid-assoicated abuse liability and physical dependence
and assess its functional effecitvenss and selectivity. Our unique set of behavioral and physiological assays in
awake, behaving non-human primates, in combination with the availability of novel buprenorphine-inspired
compounds, sets the breakthrough stage for the identification of an effective medication for opioid-induced
adverse effects and sheds light on future clinical interventions and the treatment options for opioid use
disorder.

## Key facts

- **NIH application ID:** 10359832
- **Project number:** 5R01DA053343-02
- **Recipient organization:** WAKE FOREST UNIVERSITY HEALTH SCIENCES
- **Principal Investigator:** MEI-CHUAN KO
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2022
- **Award amount:** $697,628
- **Award type:** 5
- **Project period:** 2021-03-01 → 2026-01-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10359832

## Citation

> US National Institutes of Health, RePORTER application 10359832, Buprenorphine analogs for the treatment of opioid abuse (5R01DA053343-02). Retrieved via AI Analytics 2026-05-24 from https://api.ai-analytics.org/grant/nih/10359832. Licensed CC0.

---

*[NIH grants dataset](/datasets/nih-grants) · CC0 1.0*