GlyT2 Antagonist

Opiranserin (VVZ-149) hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC₅₀s of 0.86 and 1.3 μM, respectively. Opiranserin hydrochloride shows antagonistic activity on rP2X3 (IC₅₀=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain.

Opiranserin (VVZ-149), a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC₅₀s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC₅₀=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain.

VVZ-068 is a benzamide derivative and also a GlyT2/5HT2A antagonist. VVZ-068 alleviates neuropathic mechanical hyperalgesia in a rat model of mechanical allodynia. VVZ-068 is applicable for pain-related research.