# Glycosylated Endomorphin Analogs for Treatment of Opioid Use Disorder (OUD)

> **NIH NIH U18** · TULANE UNIVERSITY OF LOUISIANA · 2021 · $241,450

## Abstract

Opioids acting at the mu opioid receptor (MOR) remain the gold standard for moderate to
severe pain relief, but serious side effects, particularly abuse liability, limit their use. The opioid
epidemic has grown steadily in the past two decades, resulting in 130 deaths per day.
Medications for treatment of opioid use disorder (OUD), particularly methadone and
buprenorphine, have been helpful, but also have limitations. In addition to issues of compliance,
they have reinforcing effects themselves, contributing to the need for close regulation. In this
program, we will test modifications of a core pharmacophore of endomorphin analogs that has
been shown to provide pain relief comparable to morphine while exhibiting reduction of several
side effects, including abuse liability. In this program we will synthesize and screen glycosylated
analogs of endomorphin with the goal of enhancing the blood-brain-barrier penetration and oral
activity of the compounds. We will test them for antinociception and their ability to block the
rewarding effects of morphine. The goal of these studies is to provide proof-of-concept that
novel endomorphin analogs can provide 1.) Effective treatment of pain without rewarding
properties, reducing the initiation of OUD and 2.) Effective blockade of opioid-induced reward,
providing the basis for a novel medication for treatment of OUD.

## Key facts

- **NIH application ID:** 10107546
- **Project number:** 1U18DA052539-01
- **Recipient organization:** TULANE UNIVERSITY OF LOUISIANA
- **Principal Investigator:** James E Zadina
- **Activity code:** U18 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $241,450
- **Award type:** 1
- **Project period:** 2021-01-01 → 2022-12-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10107546

## Citation

> US National Institutes of Health, RePORTER application 10107546, Glycosylated Endomorphin Analogs for Treatment of Opioid Use Disorder (OUD) (1U18DA052539-01). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/10107546. Licensed CC0.

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