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Opiranserin
SKU
HY-109067-Get quote
Category Reference compound
Tags 5-HT Receptor;GlyT;P2X Receptor, GPCR/G Protein;Membrane Transporter/Ion Channel;Neuronal Signaling, Neurological Disease
Products Details
Product 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].
Web ID
– HY-109067
Shipping
– Room temperature
Applications
– Neuroscience-Neuromodulation
Molecular Formula
– C21H34N2O5
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.|[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.
CAS Number
– 1441000-45-8
Molecular Weight
– 394.51
SMILES
– O=C(C1=CC(OC)=C(OCCCC)C(OC)=C1)NCC2(CCOCC2)N(C)C
Clinical Information
– Phase 3
Research Area
– Neurological Disease
Solubility
– 10 mM in DMSO
Target
– 5-HT Receptor;GlyT;P2X Receptor
Isoform
– 5-HT2 Receptor;GlyT2;P2X3 Receptor
Pathway
– GPCR/G Protein;Membrane Transporter/Ion Channel;Neuronal Signaling
Product type
– Reference compound
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