The G Protein Signal-Biased Compound TRV130; Structures, Its Site of Action and Clinical Studies.
CURRENT TOPICS IN MEDICINAL CHEMISTRY(2020)
Abstract
Opioid agonists elicit their analgesic action mainly via mu opioid receptors; however, their use is limited because of adverse events including constipation and respiratory depression. It has been shown that analgesic action is transduced by the G protein-mediated pathway whereas adverse events are by the D-arrestin-mediated pathway through mu opioid receptor signaling. The first new-generation opioid TRV130, which preferentially activates G protein- but not beta-arrestin-mediated signal, was constructed and developed to reduce adverse events. TRV130 and other G protein-biased compounds tend to elicit desirable analgesic action with less adverse effects. In clinical trials, the intravenous TRV130 (oliceridine) was evaluated in Phase I, II and III clinical studies. Here we review the discovery and synthesis of TRV130, its main action as a novel analgesic having less adverse events, its up-to-date status in clinical trials, and additional concerns about TRV130 as demonstrated in the literature.
MoreTranslated text
Key words
mu Opioid receptors,TRV130,Oliceridine,Biased ligands,Adverse beta-arrestin effects,Agonises
AI Read Science
Must-Reading Tree
Example
![](https://originalfileserver.aminer.cn/sys/aminer/pubs/mrt_preview.jpeg)
Generate MRT to find the research sequence of this paper
Chat Paper
Summary is being generated by the instructions you defined