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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[1][2][3]. | [in vivo]
Opiranserin (25 mg/kg, s.c.) effectively reduced mechanical allodynia and pain-related behaviors with efficacy comparable to 3 mg/kg Morphine[3].
Opiranserin (80 mg/kg, p.o.) reduced mechanical allodynia in a rat SNL model[4]. | [IC 50]
GlyT2: 0.86 μM (IC50); P2X3 Receptor; rP2X3: 0.87 μM (IC50); 5-HT2A Receptor: 1.3 μM (IC50) | [References]
[1] Oh J, et al. Safety, Tolerability, and Pharmacokinetic Characteristics of a Novel Nonopioid Analgesic, VVZ-149 Injections in Healthy Volunteers: A First-in-Class, First-in-Human Study. J Clin Pharmacol. 2018 Jan;58(1):64-73. DOI:10.1002/jcph.973
[2] Nedeljkovic SS, et al. Randomised, double-blind, parallel group, placebo-controlled study to evaluate the analgesic efficacy and safety of VVZ-149 injections for postoperative pain following laparoscopic colorectal surgery. BMJ Open. 2017 Feb 17;7(2):e011035. DOI:10.1136/bmjopen-2016-011035
[3] Pang MH, et al. A series of case studies: practical methodology for identifying antinociceptive multi-target drugs. Drug Discov Today. 2012 May;17(9-10):425-34. DOI:10.1016/j.drudis.2012.01.003
[4] Christopher L Cioffi. Inhibition of Glycine Re-Uptake: A Potential Approach for Treating Pain by Augmenting Glycine-Mediated Spinal Neurotransmission and Blunting Central Nociceptive Signaling. Biomolecules. 2021 Jun 10;11(6):864. DOI:10.3390/biom11060864 |
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