Evolution and challenges of opioids in pain management: Understanding mechanisms and exploring strategies for safer analgesics

This article explores the mechanisms of opioid activity in cells, emphasizing the role of biased agonism in the analgesic and adverse effects of opioids. We further reviewed strategies to mitigate the side effects, including the development of biased agonists targeting G-proteins, exploration of opioid receptor heterodimers, allosteric activation, and selective targeting of receptor splice variants. Insights into the sodium channel ’s role and bitopic modulators also offer new avenues for drug design. The quest to develop safer and more effective analgesics while minimizing adverse effects drives ongoing research. The comprehensive understanding of opioid receptors and innovative strategies offer hope for addressing the opio id crisis and advancing pain management paradigms.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research