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SR-17018 is a novel, small molecule G protein-biased agonist of the mu-opioid receptor (μ-OR). Developed by researchers at Scripps Research, it is designed to selectively activate G protein signaling pathways while minimizing the recruitment of β-arrestin2, a mechanism hypothesized to reduce typical opioid-related adverse effects such as respiratory depression and gastrointestinal dysfunction. Preclinical studies in mouse models have demonstrated that SR-17018 provides potent, long-lasting antinociception with a significantly wider therapeutic window compared to traditional opioids like morphine and oxycodone. Furthermore, SR-17018 has shown the ability to restore the antinociceptive efficacy of morphine in tolerant animals and attenuate symptoms of morphine withdrawal, although it still exhibits some rewarding properties and the potential for physical dependence upon chronic administration.
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