SR-15099, also known as SR 2.0, is an atypical opioid and a close analogue of SR-17018 and brorphine. It is the analogue of SR-17018 in which the chlorine atom on the benzyl ring is replaced by a bromine atom. The compound is a non-competitive partial biased agonist of the mu-opioid receptor, like SR-17018. In animal studies it has robust analgesic effects while producing minimal respiratory depression or hyperlocomotion, which is why it is of interest as a model of opioid pain relief with fewer of the usual dangers. It was first described in the scientific literature by Laura M. Bohn and colleagues by 2017. It is a research compound; the source reports animal results only and describes no approved medical use.
Facts
Drug ClassPartial agonist of the mu opioid receptor, G protein-biased 2 Mechanism of ActionNoncompetitive biased agonist at the mu-opioid receptor 3 Mechanism of Action Sources
1. SR-15099 (Wikipedia)
2. Biased mu opioid receptor agonists SR-17018 and SR-14968 (PMC8640941)
Results, brainstem GTPγS assay
SR-15099 acts as a partial agonist relative to DAMGO in the brainstem GTPγS assay
Introduction, G protein signaling preference
partial agonists promoting a G protein signaling preference (SR-17018, SR-15098, and SR-15099)
View the Source3. Hyperactivity in Mice Induced by Opioid Agonists with Partial Intrinsic Efficacy and Biased Agonism Administered Alone and in Combination with Morphine (2023)
Abstract, conclusion
intrinsic efficacy measured at the receptor level is not directly proportional to drug efficacy
Abstract, biased agonist sentence
the noncompetitive biased agonists SR-17018 and SR-15099 produce submaximal hyperactivity.
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