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Opiranserin is a non-opioid analgesic.1 It is an inhibitor of glycine transporter 2 (GlyT2; IC50 = 0.86 µM) and an antagonist of the serotonin (5-HT) receptor subtype 5-HT2A and the purinergic P2X3 receptor (IC50s = 1.3 and 0.87 µM, respectively). In vivo, opiranserin reduces mechanical allodynia in a rat model of neuropathic pain induced by spinal nerve ligation (ED50 = 80 mg/kg). Formulations containing opiranserin have been used in the treatment of acute postoperative pain.
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1. A series of case studies: Practical methodology for identifying antinociceptive multi-