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Opioids Analgesics and Antagonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
R. Rachana, Tanya Gupta, Saumya Yadav, Manisha Singh
According to recent studies, opioid-induced analgesia is a result of MOR signaling through the G protein, while the side effects, are conferred via β-arrestin pathway (Manglik et al., 2016). Some of these various new structure-based alternatives to morphine opioid analgesics are BU08028, PZM21, and NFEPP and so on. These compounds act only on the analgesics pathway and therefore, have shown minimal side effects like respiratory regression, sedation, constipation, addictiveness, and opioid dependence (Ding et al., 2016; Manglik et al., 2016; Chan et al., 2017). These compounds are still in trials and might become great alternatives to the conventional opioid drugs in future.
Current strategies toward safer mu opioid receptor drugs for pain management
Published in Expert Opinion on Therapeutic Targets, 2019
Aliza T. Ehrlich, Brigitte L. Kieffer, Emmanuel Darcq
Another approach is to take advantage of buprenorphine’s mixed pharmacology, which has been proposed to exert agonism at mu, with also weak agonism at the NOP, inverse agonism at kappa and antagonism at delta opioid receptors [26]. Recently, a buprenorphine analogue was developed with bifunctionality, at MOR and the NOP receptor, as a potential non-addictive analgesic [71]. A translational study in primates, demonstrates that BU08028 induces robust analgesia with less reinforcing effects as compared to cocaine, remifentanil or buprenorphine and no respiratory depression was observed at 30-fold higher than effective analgesic doses [72,73]. The combination of an exceptional pharmacological and behavioral profile for buprenorphine should inspire future studies to identify the structural components, cellular spatiotemporal signaling dynamics and physiological responses of buprenorphine’s effects. With these mechanistic insights in hand, perhaps, modifications on buprenorphine may produce an innovative opioid with excellent therapeutic profile for pain management.