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- 2018
Biased agonism: the quest for the analgesic holy grailDOI: 10.1097/PR9.0000000000000650 Keywords: Functional selectivity, Bias, Opioid, Signaling Abstract: Opioids alleviate pain, but adverse effects severely limit their usefulness. To solve this problem, biased ligands favoring 1 signaling pathway downstream of the μ-opioid receptor over another are being developed. In the target article, the authors synthesize compounds that preferentially activate G-protein or β-arrestin signaling. They find that increased bias towards G-protein signaling produces better antinociception with minimal side effects in mice models. G-protein–biased opioids may provide a safer treatment strategy
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