SR 17018 is an orally bioavailable and brain-penetrant agonist of μ-opioid receptors.
CAS：2134602-45-0
分子式：C19H18Cl3N3O
分子量：410.7
纯度：98%
存储：Store at -20°C

Background:

SR 17018 is an orally bioavailable and brain-penetrant agonist of μ-opioid receptors. It is functionally selective for G protein-coupled receptor signaling (EC50 = 97 nM for GTPγS binding in CHO cells expressing μ-opioid receptors) over β-arrestin 2 recruitment (EC50 = >10,000 nM) at the μ-opioid receptor. SR 17018 increases latency to withdraw in the hot plate and warm water tail-flick assay (ED50s = 6.9 and 7.7 mg/kg, respectively) without inducing respiratory depression in mice when administered at doses up to 48 mg/kg. SR 17018 was designed for this biased agonism at the μ-opioid receptor to potentially widen the therapeutic window and reduce adverse effects of μ-opioid receptors, such as respiratory depression.