SR 17018

SR 17018

CAT N°: 24480
Price:

From 75.00 63.75

SR 17018 is an orally bioavailable and brain-penetrant agonist of ?-opioid receptors.{40627} It is functionally selective for G protein-coupled receptor signaling (EC50 = 97 nM for GTP?S binding in CHO cells expressing ?-opioid receptors) over ?-arrestin 2 recruitment (EC50 = >10,000 nM) at the ?-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 ?-opioid receptor to potentially widen the therapeutic window and reduce adverse effects of ?-opioid receptors, such as respiratory depression.

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