Cebranopadol

Cebranopadol is an agonist of nociceptin-, µ-, ĸ-, and δ-opioid receptors (K_is = 0.9, 0.7, 2.6, and 18 nM, respectively).¹ It is greater than 100-fold selective for these receptors over a panel of more than 100 ion channels, neurotransmitter transporters, receptors, and enzymes, but does bind to the serotonin (5-HT) receptor subtype 5-HT_5A with a K_i value of 8.7 nM. Cebranopadol inhibits nociceptin-, DAMGO-, and SNC 80-induced GTPɣS binding in CHO cells expressing nociceptin-, µ-, and δ-opioid receptors, respectively (EC₅₀s = 13, 1.2, and 110 nM, respectively), as well as U69,593-induced GTPɣS binding in HEK293 cells expressing the ĸ-opioid receptor (EC₅₀ = 17 nM). It increases the paw withdrawal threshold in rat models of bone cancer pain and streptozotocin-induced diabetic neuropathy (ED₅₀s = 3.6 and 0.5 µg/kg, respectively, i.v.). Cebranopadol also increases paw weight bearing on the ipsilateral side in a rat model of arthritis induced by complete Freund's adjuvant (CFA) and M. tuberculosis (ED₅₀ = 5.5 µg/kg, i.v.).

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1. Linz, K., Christoph, T., Tzschentke, T.M., et al. Cebranopadol: A novel potent analgesic nociceptin/orphanin FQ peptide and opioid receptor agonist. J. Pharmacol. Exp. Ther. 349(3), 535-548 (2014).