Pain is a common symptom accompanying several clinical conditions and causes serious distress to patients. Addressing pain management is an important aspect of disease treatment, including cancer therapy. Opioid analgesics used to manage pain in human and veterinary medicine have been associated with substance dependence and other adverse effects, thereby limiting their application. Thus, the development of opioid analgesics with good safety profiles with minimal adverse effects and no addictive effects, is presently the focus of pain research. As a new potential analgesic, (2S)-2-[(5R,6R,7R,14S)-N-cyclopropylmethyl-4,5-epoxy-6,14-ethano-3-hydroxy-6-methoxymorphinan-7-yl]-3,3-dimethylpentan-2-ol (BU08028) has fewer adverse effects than other analgesics and is expected to be a safer alternative. In this review, we discuss the development of the opioid analog BU08028 and summarize its analgesic effects and biological characteristics, including efficiency, safety, and tolerance. Furthermore, we elaborate on studies showing the bifunctional effect of BU08028, which targets both mu opioid peptide and nociceptin-orphanin FQ peptide receptors, as well as the unique advantages of using BU08028 over single-target opioid agonists. Previous studies have suggested that BU08028 can not only weaken the reward and abuse effects of opioids and other drugs, but also enhance the anti-nociceptive effect of the mu opioid peptide receptors, making it a potent analgesic. Besides, we describe studies suggesting that BU08028 inhibits the effects of alcohol, making it a candidate drug for the management of alcohol addiction. Our review suggests that BU08028 is a potential novel medicine for managing pain and addiction.
Keywords: Analgesic; Analgesic effect; BU08028; Opioid; Pain management.
Copyright © 2021. Published by Elsevier B.V.