Opioid use disorders (OUD) pose an imminent threat to human health worldwide with approximately 2.1 million Americans suffering from this epidemic. Along with the analgesia produced by opioids, their ability to cause euphoria, due to activation of the mu-opioid receptor (MOR) in several regions of the brain, often leads to opioid misuse. Currently, detoxification and maintenance therapy are the two mostly used approaches to treat OUD. Methadone, buprenorphine and naltrexone (NTX) are first-line opioid medicines approved by the US Food and Drug Administration (FDA) for OUD. However, they carry some concerning side effects like the withdrawal symptoms precipitated by NTX and naloxone (NLX), including abdominal cramps, nausea/vomiting, diarrhea, muscle aches, anxiety, confusion, and extreme sleepiness. High doses of these drugs are also reported to show hepatotoxicity, cardiovascular and pulmonary problems. Thus, there is an urgent need to develop highly potent, efficacious, and selective MOR ligands with minimum side effects as OUD medications. In our lab, NAQ was identified as a selective, high potency and low efficacy MOR partial agonist. NAQ carries acceptable ADMET properties and improved oral bioavailability over naloxone (NLX) and naltrexone (NTX). At the in vivo level, NAQ displayed potent inhibition of the analgesic effect of morphine while precipitating fewer withdrawal symptoms in morphine dependent mice than NLX and NTX. In self administration studies, NAQ (10 and 32 mg/kg/day) produced behavioral reallocation away from heroin and towards the alternative nondrug food reinforcer. Overall, NAQ seems a promising molecule for developing novel opioid abuse and addiction therapeutic agents. Future studies including formulation, oral effective dose for OUD treatment, in vivo metabolism profiling, acute and chronic toxicities are warranted.