Oliceridine – Mechanism of Action and Synthesis

Oliceridine is an opioid medication that was approved by the FDA for the treatment of moderate to severe acute pain in adults. The medication is indicated for short-term intravenous use in hospitals and other controlled clinical settings. Disease: CNS Target: μ-opioid receptor (MOR). Mechanism of Action: G protein-biased μ-opioid receptor agonist. Chemistry section: Retrosynthesis & Forward Synthesis. Opioids are the most effective drugs for the treatment of acute and chronic pain, and they occupy the largest market share of analgesic medications. Medical uses of opioids for pain relief include opioid alkaloids such as morphine and synthetic opioids like fentanyl. Although opioids are potent painkillers, they also result in severe adverse effects such as addiction, respiratory suppression, and constipation, thus limiting their clinical use. In this video, I talk about the mechanism of action of oliceridine and its chemical synthesis. References: 1. J. Med. Chem. 2013, 56, 8019. 2. Cell. 2022, 185, 4361. 3. Sci. Signal. 13, eaaz3140 (2020) 4. Br J Pharmacol. 2020, 177, 2923. 5. J. Med. Chem. 2022, 65, 9607.

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