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Opiranserin

CAT: 0804-HY-109067Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-109067Size:1 Each
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Description
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].
CAS Number
1441000-45-8
Product Name Alternative
VVZ-149
UNSPSC
12352005
Hazard Statement
H302-H315-H319-H335
Target
5-HT Receptor; GlyT; P2X Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein; Membrane Transporter/Ion Channel; Neuronal Signaling
Applications
Neuroscience-Neuromodulation
Field of Research
Neurological Disease
Assay Protocol
https://www.medchemexpress.com/opiranserin.html
Solubility
10 mM in DMSO
Smiles
O=C(C1=CC(OC)=C(OCCCC)C(OC)=C1)NCC2(CCOCC2)N(C)C
Molecular Formula
C21H34N2O5
Molecular Weight
394.51
Precautions
P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362-P403+P233-P405-P501
References & Citations
[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.|[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.|[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.|[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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Phase 3
Isoform
5-HT2 Receptor; GlyT2; P2X3 Receptor; α-1 microglobulin

Alternative Products

CatalogName
GTR19203768-01Opiranserin
MBS3617430-01Opiranserin hydrochloride

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