Opiranserin  (Synonyms: VVZ-149)

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

394.51

C₂₁H₃₄N₂O₅

1441000-45-8

O=C(C1=CC(OC)=C(OCCCC)C(OC)=C1)NCC2(CCOCC2)N(C)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]