An orally available antagonist of the nociceptin receptor opioid receptor like -1 (ORL-1), with potential analgesic activity. Upon oral administration, cebranopadol binds to ORL-1 and prevents its interaction with nociceptin. This leads to a decrease of nociceptin/ORL-1-mediated signaling and interferes with the sensation of pain, which results in an analgesic effect. Nociceptin is a neuropeptide involved in the regulation of pain.