1441000-45-8

1441000-45-8 structure

Name: Opiranserin
Chemical Name: opiranserin
CAS Number: 1441000-45-8
Molecular Formula: C₂₁H₃₄N₂O₅
Molecular Weight: 394.505
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2020-01-12 02:57:50
Modify Date: 2024-01-06 11:52:27
Opiranserin (VVZ-149, VVZ-000149) is a potent, selective, mixed glycine GlyT2 transporter blocker (IC50= 0.86 uM), purine P2X3 receptor antagonist (IC50=0.87 uM) and serotonin 5-HT2A receptor antagonist (IC50=1.3 uM); demonstrates analgesic efficacy for postoperative pain. Pain Phase 2 Clinical

Name	opiranserin
Synonyms	4-Butoxy-N-{[4-(dimethylamino)tetrahydro-2H-pyran-4-yl]methyl}-3,5-dimethoxybenzamide Benzamide, 4-butoxy-N-[[4-(dimethylamino)tetrahydro-2H-pyran-4-yl]methyl]-3,5-dimethoxy- opiranserin

Description	Opiranserin (VVZ-149, VVZ-000149) is a potent, selective, mixed glycine GlyT2 transporter blocker (IC50= 0.86 uM), purine P2X3 receptor antagonist (IC50=0.87 uM) and serotonin 5-HT2A receptor antagonist (IC50=1.3 uM); demonstrates analgesic efficacy for postoperative pain. Pain Phase 2 Clinical
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> GlyT Signaling Pathways >> Membrane Transporter/Ion Channel >> P2X Receptor Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> GlyT
Target	5-HT2A Receptor:1.3 μM (IC50) GlyT2:0.86 μM (IC50) rP2X3:0.87 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. [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.