%0 Journal Article
%T Biased agonism: the quest for the analgesic holy grail
%A M. Alexander Stanczyk
%A Ram Kandasamy
%J Archive of "Pain Reports".
%D 2018
%R 10.1097/PR9.0000000000000650
%X Opioids alleviate pain, but adverse effects severely limit their usefulness. To solve this problem, biased ligands favoring 1 signaling pathway downstream of the ¦Ì-opioid receptor over another are being developed. In the target article, the authors synthesize compounds that preferentially activate G-protein or ¦Â-arrestin signaling. They find that increased bias towards G-protein signaling produces better antinociception with minimal side effects in mice models. G-protein¨Cbiased opioids may provide a safer treatment strategy
%K Functional selectivity
%K Bias
%K Opioid
%K Signaling
%U https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5999417/