# Characterization GPR83 and identification of small molecule ligands targeting this receptor for the treatment of substance use disorders.

> **NIH NIH U18** · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · 2021 · $247,028

## Abstract

Project Summary
Opioids are powerful analgesics clinically used in treatment of chronic pain; they are also rewarding, and thus
have high risk for abuse and dependence. Up to 25% of all patients receiving long-term opioid therapy struggle
with opioid addiction, which is especially concerning considering that more than 191 million prescriptions for
opioids were dispensed to patients in 2017 leading to the current opioid crisis. This has led to the search of novel
strategies/therapeutic targets to treat pain. Hypothalamic neuropeptide receptors have emerged as potential
targets for development of therapeutics for the treatment of substance use disorders. With the intent of identifying
additional neuropeptide receptor systems, we recently deorphanized the hypothalamic receptor GPR83 as a
receptor for an abundant neuropeptide, PEN. GPR83 is expressed in the reward centers of the brain. Also, local
knock-down of GPR83 leads to attenuation of the rewarding effects of morphine making GPR83 a potential target
for the development of novel therapeutics. The studies in this application are to characterize a recently identified
small molecule antagonist targeting GPR83 with the intent of identifying drugs for the treatment of substance
use disorders. These studies are highly significant since they are likely to open novel therapeutic possibilities for
the treatment of addiction.

## Key facts

- **NIH application ID:** 10104088
- **Project number:** 1U18DA052345-01
- **Recipient organization:** ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI
- **Principal Investigator:** Lakshmi A Devi
- **Activity code:** U18 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $247,028
- **Award type:** 1
- **Project period:** 2020-12-01 → 2021-11-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10104088

## Citation

> US National Institutes of Health, RePORTER application 10104088, Characterization GPR83 and identification of small molecule ligands targeting this receptor for the treatment of substance use disorders. (1U18DA052345-01). Retrieved via AI Analytics 2026-05-24 from https://api.ai-analytics.org/grant/nih/10104088. Licensed CC0.

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